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459 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.EBI
Huazhong University of Science and Technology
Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.EBI
Dipartimento di Farmacia Universit£ di Napoli"Federico II"
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.EBI
Huazhong University of Science and Technology
Bifunctional compounds targeting both D2 and non-a7 nACh receptors: design, synthesis and pharmacological characterization.EBI
Universit£ degli Studi di Milano
Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent.EBI
Jagiellonian University Medical College
Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.EBI
Universit£ degli Studi di Chieti Gabriele D'Annunzio
Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT1A receptor functional profile.EBI
Jagiellonian University Medical College
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.EBI
Intra-Cellular Therapies Inc
Molecular similarity, quantitative chirality, and QSAR for chiral drugs.EBI
University of Oxford
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.EBI
University of Santiago de Compostela
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.EBI
Universidade Federal de Goi£s
Spiropiperidines as high-affinity, selective sigma ligands.EBI
Merck Sharp and Dohme Research Laboratories
Benz[f]isoquinoline analogues as high-affinity sigma ligands.EBI
Merck Sharp and Dohme Research Laboratories
Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor.EBI
Merrell Dow Research Institute
The role of QSAR in dopamine interactions.EBI
Pomona College
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.EBI
University of Li£ge
Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines.EBI
University of Lausanne
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.EBI
University of Santiago
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.EBI
Janssen-Cilag S.A.
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.EBI
Janssen-Cilag S.A.
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.EBI
Organon Research and Development Group
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.EBI
Universidad de Santiago de Compostela
Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.EBI
University of Bologna
Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.EBI
TBA
Structure-activity relationship study of N6-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine analogues: development of highly selective D3 dopamine receptor agonists along with a highly potent D2/D3 agonist and their pharmacological characterizatioEBI
Wayne State University
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.EBI
Gedeon Richter Plc
Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1.EBI
Medical University of Warsaw
Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors.EBI
Harvard Medical School
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.EBI
European Research Centre for Drug Discovery and Development (NatSynDrugs)
Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.EBI
Universita degli Studi di Bari
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.EBI
The University of Mississippi
Advances in development of dopaminergic aporphinoids.EBI
Chinese Academy of Sciences
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.EBI
Taisho Pharmaceutical Co., Ltd
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.EBI
Purdue University
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.EBI
Universit£ degli Studi di Urbino Carlo Bo
Designed multiple ligands. An emerging drug discovery paradigm.EBI
Organon Laboratories
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.EBI
National Institute on Drug Abuse-Intramural Research Program
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.EBI
Universit£ di Modena and Reggio Emilia
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects.EBI
Daiichi Suntory Biomedical Research Co., Ltd
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.EBI
Abbott Laboratories
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.EBI
Dainippon Pharmaceutical Co., Ltd
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.EBI
H. Lundbeck A/S
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.EBI
Universit£ di Siena
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.EBI
Universit£ degli Studi di Sassari
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.EBI
Universit£ degli Studi di Siena
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.EBI
Eli Lilly and Company
Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.EBI
CoCensys Inc
Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists.EBI
University of Maastricht
Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.EBI
Suntory Biomedical Research Limited
CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors.EBI
University of Texas
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).EBI
University Centre for Pharmacy
7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.EBI
University of Bonn
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.EBI
Taisho Pharmaceutical Company Ltd
Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.EBI
Wyeth-Ayerst Research
Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.EBI
Taisho Pharmaceutical Company Ltd
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.EBI
University of Minnesota
N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.EBI
University of Crete
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.EBI
Universita' di Siena
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.EBI
R. W. Johnson Pharmaceutical Research Institute
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.EBI
University of Catania
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.EBI
Yamanouchi Pharmaceutical Company, Ltd
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.EBI
Wyeth-Ayerst Research Laboratories
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.EBI
Abbott Laboratories
Structure-activity relationships of a series of substituted benzamides: potent D2/5-HT2 antagonists and 5-HT1a agonists as neuroleptic agents.EBI
Glaxo Wellcome Inc.
Comparative molecular field analysis-based prediction of drug affinities at recombinant D1A dopamine receptors.EBI
VA Medical Center
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.EBI
Universit£ di Bari
Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives.EBI
Universit£ di Bari
Synthesis, resolution, and preliminary evaluation of trans-2-amino-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes and related derivatives as dopamine receptors ligands.EBI
Universit£ di Camerino
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.EBI
Hoechst Marion Roussel Inc
1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3.EBI
Universit£ di Bari
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).EBI
Hoechst-Roussel Pharmaceuticals Inc
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.EBI
Neurogen Corporation
(+/-)-(N-alkylamino)benzazepine analogs: novel dopamine D1 receptor antagonists.EBI
National Institutes of Health
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.EBI
R. W. Johnson Pharmaceutical Research Institute
Piperazinylalkyl heterocycles as potential antipsychotic agents.EBI
R. W. Johnson Pharmaceutical Research Institute
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 2. Effects of 8-amino nitrogen substitution on serotonin receptor binding and pharmacology.EBI
Upjohn Laboratories
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.EBI
H. Lundbeck A/S
Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.EBI
CIFA Universidad de Navarra
Studies of the active conformation of a novel series of benzamide dopamine D2 agonists.EBI
Warner-Lambert Company
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.EBI
University of G£teborg
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.EBI
Albany Molecular Research, Inc.
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.EBI
Upjohn Laboratories
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.EBI
University of Pennsylvania
Conformationally restricted analogues of remoxipride as potential antipsychotic agents.EBI
Burroughs Wellcome Co.
Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo.EBI
Medicinaregatan
Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans.EBI
H. Lundbeck A/S
Synthesis and pharmacological evaluation of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for a novel receptor with sigma-like neuromodulatory activity.EBI
University of North Carolina
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.EBI
University of Pennsylvania
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.EBI
Upjohn Laboratories
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.EBI
Searle Research and Development
Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.EBI
Upjohn Laboratories
Pyrrole mannich bases as potential antipsychotic agents.EBI
R. W. Johnson Pharmaceutical Research Institute
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.EBI
Bristol-Myers Squibb Co.
Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl)ethylamine and N,N-dialkyl derivatives as dopamine receptor ligands.EBI
University of Camerino
Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine.EBI
Universit£ di Bari
Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model.EBI
University of Lund
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine.EBI
Warner-Lambert Company
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.EBI
Centre de Recherches de Vitry Alfortville Rh£ne-Poulenc Rorer
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.EBI
Virginia Commonwealth University
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.EBI
Astra Research Centre AB
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.EBI
Hoechst-Roussel Pharmaceuticals Inc
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds.EBI
Dainippon Pharmaceutical Company, Ltd.
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.EBI
Abbott Laboratories
Antidopaminergic effects of the stereoisomers of N-[(1-alkyl-2- pyrrolidinyl)methyl]-5-sulfamoylbenzamides and -2,3-dihydrobenzofuran-7-carboxamides.EBI
Yoshitomi Pharmaceutical Industries Ltd
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.EBI
Warner-Lambert Company
R and S enantiomers of 11-hydroxy- and 10,11-dihydroxy-N-allylnoraporphine: synthesis and affinity for dopamine receptors in rat brain tissue.EBI
Northeastern University
Synthesis and dopamine receptor affinities of 2-(4-fluoro-3- hydroxyphenyl)ethylamine and N-substituted derivatives.EBI
University of Camerino
trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist.EBI
Purdue University
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.EBI
Astra Research Centre AB
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.EBI
Abbott Laboratories
Synthesis and structural requirements of N-substituted norapomorphines for affinity and activity at dopamine D-1, D-2, and agonist receptor sites in rat brain.EBI
Northeastern University
4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.EBI
Warner-Lambert Company
Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents.EBI
University of Pennsylvania
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.EBI
National Institute of Digestive
5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine.EBI
College of Pharmacy University of Iowa
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.EBI
Bristol-Myers Company
Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents.EBI
Wyeth-Ayerst Research
Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics.EBI
Eli Lilly and Company
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.EBI
University of G£teborg
Substituted benzamides. 1. Potential nondopaminergic antagonists of chemotherapy-induced nausea and emesis.EBI
Bristol-Myers Company
Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies.EBI
Wyeth-Ayerst Research
Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.EBI
University of Pennsylvania
Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition.EBI
University of Lund
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.EBI
H. Lundbeck A/S
Synthesis and pharmacology of trans-4-n-propyl-3,4,4a,10b-tetrahydro-2H,5H-1-benzopyrano[4,3-b ]-1,4-oxazin-7- and -9-ols: the significance of nitrogen pKa values for central dopamine receptor activation.EBI
State University of Groningen
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.EBI
Vanderbilt University
Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands.EBI
University of North Carolina
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.EBI
TBA
N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors.EBI
University of G£teborg
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.EBI
Duphar Research Laboratories
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.EBI
Istituto Superiore di Sanit£
Antipsychotic activity of substituted gamma-carbolines.EBI
Wyeth Laboratories, Inc.
Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives.EBI
TBA
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.EBI
TBA
Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics.EBI
TBA
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.EBI
TBA
Synthesis, resolution, absolute stereochemistry, and enantioselectivity of 3',4'-dihydroxynomifensine.EBI
TBA
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.EBI
Eli Lilly and Company
New generation dopaminergic agents. Part 8: heterocyclic bioisosteres that exploit the 7-OH-2-(aminomethyl)chroman D(2) template.EBI
Wyeth-Ayerst Research Laboratories
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands.EBI
Universidad de Alcal£
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.EBI
Abbott Laboratories
A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects.EBI
Institute for Bio-Medical Research
A novel series of N-(hexahydro-1,4-diazepin-6-yl) and N-(hexahydroazepin- 3-yl)benzamides with high affinity for 5-HT3 and dopamine D2 receptors.EBI
Dainippon Pharmaceutical Co., Ltd
 
Synthesis and pharmacological activity of a macrocyclic benzamideEBI
TBA
 
Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibitionEBI
TBA
 
Dopamine autoreceptor agonists: computational studies, synthesis and biological investigationsEBI
TBA
 
Synthesis and pharmacological evaluation of the enantiomers of the dopamine autoreceptor agonist PD 135385EBI
TBA
 
(5S)-3-aryl-5-(1-piperidinylmethyl)-2-oxazolidinones, a new class of potential neuroleptics with a high affinity for sigma receptorsEBI
TBA
 
Novel 4,5,6,7-tetrahydrobenzothiazole dopamine agonists display very low stereoselectivity in their interaction with dopamine receptors.EBI
TBA
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.EBI
Universit£ degli Studi di Siena
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation.EBI
Jagiellonian University Medical College
New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation.EBI
Universit£ di Napoli"Federico II"
New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage.EBI
Universidad Complutense de Madrid
New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists.EBI
University of Tartu
Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.EBI
Universit£ di Napoli Federico II
1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis.EBI
Pfizer Inc
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.EBI
University of Catania
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI
National Institute of Mental Health
Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol.EBI
Wayne State University
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.EBI
Universita di Siena
New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation.EBI
Universit£ di Napoli Federico II
Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity.EBI
Jagiellonian University Medical College
Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives.EBI
Jagiellonian University Medical College
Tetrahydroisoquinolines as dopaminergic ligands: 1-Butyl-7-chloro-6-hydroxy-tetrahydroisoquinoline, a new compound with antidepressant-like activity in mice.EBI
Universidad de Valencia
N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists.EBI
University of Tartu
Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol: effect on affinity and selectivity for dopamine D3 receptor.EBI
Wayne State University
Displacement Activity of Bisbenzylisoquinoline Alkaloids at Striatal 3H-SCH 23390 and 3H-Raclopride Binding SitesEBI
TBA
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.EBI
TBA
 
Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity.EBI
TBA
 
(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonistsEBI
TBA
 
5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like propertiesEBI
TBA
 
The synthesis and evaluation of the major metabolites of mazapertineEBI
TBA
 
(E) and (Z)-3-Styrylpiperidines as sigma ligandsEBI
TBA
 
1-(2-METHOXYPHENYL)-4-ALKYLPIPERAZINES: EFFECT OF THE N-4 SUBSTITUENT ON THE AFFINITY AND SELECTIVITY FOR DOPAMINE D4 RECEPTOREBI
TBA
 
2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT1A receptor ligandEBI
TBA
 
Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)EBI
TBA
 
N-(2-pyrrolidinylmethyl)benzoxazine-8-carboxamides exhibiting high affinities for All of D2, 5-HT1 A, and 5-HT2 receptorsEBI
TBA
 
Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic propertiesEBI
TBA
 
Novel HO-DPAT (hydroxy-2-dipropylaminotetralin) isomers: Stereoselective synthesis and receptor binding studiesEBI
TBA
 
Enhancement of binding of quaternary ammonium derivatives of chlorpromaxine to dopamine D-2 receptors by the addition of a H-bonding groupEBI
TBA
 
4-Aminomethyl chromans: dependence of serotonin and dopamine binding upon aromatic ring substitutionEBI
TBA
 
4-Aryltetrahydropyridines as selective σ ligandsEBI
TBA
 
Substituted Benzamides with Conformationally Restricted Side Chains. 3. Azabicyclo[x.y.0] derivatives as gastric prokinetic agents.EBI
TBA
 
Dopamine receptor binding properties of some 2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols with non-aromatic substituents in the 5-positionEBI
TBA
 
Synthesis and dopaminergic activity of the enantiomers of 6-methyl-4,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine (PD 128483).EBI
TBA
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.EBI
European Research Centre for Drug Discovery and Development (NatSynDrugs)
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.EBI
University of Siena
Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.EBI
Harvard Medical School
Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding characterization at D2/D3 receptors and elucidation of a pharmacophore model.EBI
Wayne State University
Design, synthesis, and evaluation of potent and selective ligands for the dopamine 3 (D3) receptor with a novel in vivo behavioral profile.EBI
University of Michigan
Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.EBI
Università di Catania
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.EBI
Harvard Medical School
Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.EBI
Wayne State University
Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines.EBI
University of Debrecen
Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines.EBI
University of Debrecen
Halogenated boldine derivatives with enhanced monoamine receptor selectivity.EBI
Universidad de Chile
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.EBI
Universidad de Valencia
Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile.EBI
Gedeon Richter Ltd
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.EBI
Harvard Medical School
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.EBI
Eli Lilly and Company
Novel sigma receptor ligands: synthesis and biological profile.EBI
University of Catania
Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation.EBI
University of Montpellier
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.EBI
Taisho Pharmaceutical Co., Ltd
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.EBI
Abbott Laboratories
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.EBI
Johann Wolfgang Goethe University
11C-labeling of n-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors.EBI
University of Milano/Bicocca
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.EBI
Università di Napoli "Federico II"
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.EBI
Friedrich-Alexander University
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.EBI
Università di Catania
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.EBI
Università di Siena
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.EBI
Merck KGaA
Indolebutylamines as selective 5-HT(1A) agonists.EBI
Merck KGaA
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.EBI
Uppsala University
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.EBI
Università di Bari
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.EBI
Wake Forest University School of Medicine
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.EBI
Cracow University of Technology
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.EBI
Yale University
Orally active oxime derivatives of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one. Synthesis and pharmacological activity.EBI
University Center for Pharmacy
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.EBI
National Institute on Drug Abuse-Intramural Research Program
Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.EBI
Universidad Complutense
Development of a presynaptic 5-HT1A antagonist.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological investigation of new equatorial (?) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.EBI
Medical University of Warsaw
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.EBI
Friedrich-Alexander University
Isoquinolinone derivatives as potent CNS multi-receptor DEBI
Jiangsu Ocean University
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.EBI
University Center for Pharmacy
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.EBI
Yale University
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.EBI
Université de Lille 2
Antiangiogenic Effect of ()-Haloperidol Metabolite II Valproate Ester [()-MRJF22] in Human Microvascular Retinal Endothelial Cells.EBI
University of Catania
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI
Pharmazeutisches Institut der Universität Freiburg
Dopamine D(3) receptor antagonists. 1. Synthesis and structure-activity relationships of 5,6-dimethoxy-N-alkyl- and N-alkylaryl-substituted 2-aminoindans.EBI
Pharmacia
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.EBI
Università Bari
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.EBI
Cracow University of Technology
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.EBI
Universidad de Navarra
Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel.EBI
AstraZeneca Pharmaceuticals LP
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI
Columbia University College of Physicians and Surgeons
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.EBI
Wake Forest University School of Medicine
Enantioselective syntheses of dopaminergic (R)- and (S)-benzyltetrahydroisoquinolines.EBI
Universidad de Valencia
1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors.EBI
Wyeth-Ayerst Research
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.EBI
University of Crete
New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects.EBI
Suntory Biomedical Research Limited
Benzimidazolone-based selective ?EBI
University of Florida
New substituted 1-(2,3-dihydrobenzo[1, 4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with alpha(2)-adrenoceptor antagonist activity.EBI
Centre de Recherche Pierre Fabre
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.EBI
CoCensys Inc
Towards the PET radiotracer for p75 neurotrophin receptor: [(11)C]LM11A-24 shows biological activity in vitro, but unfavorable ex vivo and in vivo profile.EBI
University of British Columbia
Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.EBI
University of Tokyo
Novel multifunctional dopamine DEBI
Wayne State University
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.EBI
University of Siena
New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.EBI
Wyeth-Ayerst Research Laboratories
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.EBI
Knoll Pharmaceuticals
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.EBI
CoCensys Inc
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI
University of Göteborg
Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.EBI
Cracow University of Technology
N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.EBI
POSTECH
New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.EBI
Wyeth-Ayerst Research Laboratories
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.EBI
Università di Bari
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists.EBI
Recordati S.p.A.
Synthesis and structure-activity relationships of a new model of arylpiperazines. 4. 1-[omega-(4-Arylpiperazin-1-yl)alkyl]-3-(diphenylmethylene) - 2, 5-pyrrolidinediones and -3-(9H-fluoren-9-ylidene)-2, 5-pyrrolidinediones: study of the steric requirements of the terminal amide fragment on 5-HT1A aEBI
Universidad Complutense
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).EBI
Centro de Investigación Grupo Ferrer
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.EBI
Wyeth-Ayerst Research Laboratory
Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors.EBI
Dainippon Pharmaceutical Co., Ltd
Serotonergic ergoline derivatives.EBI
Pharmacia & Upjohn
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.EBI
Wyeth-Ayerst Research Laboratories
1-[omega-(4-arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5- pyrrolidinediones as 5-HT1A receptor ligands: study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity.EBI
Universidad Complutense
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.EBI
R. W. Johnson Pharmaceutical Research Institute
Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding.EBI
Virginia Commonwealth University
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.EBI
Yamanouchi Pharmaceutical Company, Ltd
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.EBI
University of Camerino
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.EBI
University of Groningen
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.EBI
Università di Catania
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.EBI
Solvay Pharma
3-[[(4-Aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as dopamine D2 partial agonists and autoreceptor agonists.EBI
Division of Warner Lambert Company
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.EBI
University of Groningen
Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist.EBI
Universidad Complutense
Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole.EBI
H. Lundbeck A/S
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.EBI
Cracow University of Technology
(+/-)-3-[4'-(N,N-dimethylamino)cinnamyl]benzazepine analogs: novel dopamine D1 receptor antagonists.EBI
National Institutes of Health
Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships.EBI
Warner-Lambert Company
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.EBI
Yamanouchi Pharmaceutical Company Limited
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.EBI
Pharmacia & Upjohn
Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist.EBI
University of Camerino
Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson's Disease.EBI
Wayne State University
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.EBI
Glaxo Wellcome Inc.
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.EBI
Pfizer Inc
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.EBI
Hoechst-Roussel Pharmaceuticals Inc
(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors.EBI
Wyeth Research (UK)
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.EBI
Scios Nova Inc
New indole derivatives as potent and selective serotonin uptake inhibitors.EBI
Centre de Recherches de Vitry-Alfortville
Synthesis and in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled sigma binding site.EBI
Scios Nova Inc
A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds.EBI
University of Lund
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI
Eli Lilly and Company
(S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists.EBI
University of Göteborg
Mixed 5-HT1A/D-2 activity of a new model of arylpiperazines: 1-aryl-4-[3-(1,2-dihydronaphthalen-4-yl)-n-propyl]piperazines. 1. Synthesis and structure-activity relationships.EBI
Università di Bari
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI
Solvay Duphar B.V.
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.EBI
University of Göteborg
Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.EBI
University of Maryland
Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists. Predicting selectivity with respect to dopamine D2 receptors.EBI
H. Lundbeck A/S
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.EBI
University of Liège
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.EBI
Upjohn Laboratories
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.EBI
University of Pennsylvania
2,3,9- and 2,3,11-trisubstituted tetrahydroprotoberberines as D2 dopaminergic ligands.EBI
Universidad de Valencia
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.EBI
George Washington University Medical Center
3,4-Dihydroxy- and 3,4-methylenedioxy- phenanthrene-type alkaloids with high selectivity for D2 dopamine receptor.EBI
Universidad de Valencia
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.EBI
Universidade Federal do Rio de Janeiro
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.EBI
Parke-Davis Pharmaceutical Research
6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists.EBI
Göteborg University
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.EBI
Burroughs Wellcome Company
Dopaminergic benzo[a]phenanthridines: resolution and pharmacological evaluation of the enantiomers of dihydrexidine, the full efficacy D1 dopamine receptor agonist.EBI
Purdue University
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.EBI
Hoechst-Roussel Pharmaceuticals Inc
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.EBI
R. W. Johnson Pharmaceutical Research Institute
Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics.EBI
Scios Nova Inc
C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability.EBI
Upjohn Laboratories
Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine receptor ligands.EBI
Purdue University
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes.EBI
Göteborg University
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.EBI
Università di Bari
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.EBI
Wellcome Research Laboratories
Synthesis and evaluation of 6,7-dihydroxy-2,3,4,8,9,13b-hexahydro-1H- benzo[6,7]cyclohepta[1,2,3-ef][3]benzazepine, 6,7-dihydroxy- 1,2,3,4,8,12b-hexahydroanthr[10,4a,4-cd]azepine, and 10-(aminomethyl)-9,10- dihydro-1,2-dihydroxyanthracene as conformationally restricted analogs of beta-phenyldopaminEBI
Purdue University
Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.EBI
H. Lundbeck A/S
Two new phenylpiperazines with atypical antipsychotic potential.EBI
Institute for Biological Research
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.EBI
Central Drug Research Institute
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.EBI
Pierre Fabre Research Center
Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.EBI
Universit£ di Camerino
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.EBI
Pierre Fabre Research Center
Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor.EBI
Meiji Seika Kaisha Ltd.
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.EBI
University of Bologna
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.EBI
University of Camerino
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.EBI
Universidad de Santiago
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.EBI
FAES, S.A.
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.EBI
Monash University
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.EBI
University of Camerino
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.EBI
University of Santiago de Compostela
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.EBI
Huazhong University of Science and Technology
Troponoids. 7. Chemistry and dopamine agonist activity of ciladopa and related aralkyltroponylpiperazines.EBI
TBA
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.EBI
TBA
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.EBI
Northeastern University
Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity.EBI
CNS Line
Serotonergic properties of spiroxatrine enantiomers.EBI
University of Arizona
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.EBI
Duphar Research Laboratories
Substituted benzamides with conformationally restricted side chains. 2. Indolizidine derivatives as central dopamine receptor antagonists.EBI
Beecham Pharmaceuticals Research Division
Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives.EBI
Bristol-Myers Company
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.EBI
Warner-Lambert Company
1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents.EBI
Warner-Lambert/Parke-Davis Pharmaceutical Research
Charged analogues of chlorpromazine as dopamine antagonists.EBI
TBA
Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.EBI
TBA
Synthesis and receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol.EBI
Schering-Plough Corporation
Substituted 5-amino-4,5,6,7-tetrahydroindazoles as partial ergoline structures with dopaminergic activity.EBI
Eli Lilly and Company
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
Vanderbilt University
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.EBI
McNeil Pharmaceutical and Janssen Research Foundation Worldwide
Synthesis and D2 dopaminergic activity of pyrrolidinium, tetrahydrothiophenium, and tetrahydrothiophene analogues of sulpiride.EBI
Ohio State University
Aporphines as antagonists of dopamine D-1 receptors.EBI
Eli Lilly and Company
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.EBI
Washington University
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist.EBI
Research Biochemicals Inc.
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study.EBI
Astra Research Centre AB
Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues.EBI
Northeastern University
Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model.EBI
University of Lund
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
Vanderbilt University
Synthesis and dopamine agonist properties of (+-)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano [4,3-b]-1,4-oxazin-9-ol and its enantiomers.EBI
Warner-Lambert Company
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.EBI
University of California
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists.EBI
H. Lundbeck A/S
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.EBI
Pfizer Inc
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.EBI
Istituto Superiore di Sanità
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.EBI
Virginia Commonwealth University
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity sigma receptor ligands.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.EBI
Abbott Laboratories
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.EBI
Universit£ di Catania
Stereoisomeric probes for the D1 dopamine receptor: synthesis and characterization of R-(+) and S-(-) enantiomers of 3-allyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its 6-bromo analogue.EBI
Research Biochemicals Inc.
Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.EBI
University of Pennsylvania
6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists.EBI
University of Göteborg
Synthesis and dopaminergic activity of some 3-(1,2,3,6-tetrahydro-1-pyridylalkyl)indoles. A novel conformational model to explain structure-activity relationships.EBI
E. Merck Darmstadt
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.EBI
Hoechst-Roussel Pharmaceuticals Inc
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.EBI
H. Lundbeck A/S
Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.EBI
H. Lundbeck A/S
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.EBI
H. Lundbeck A/S
(Aminoalkoxy)chromones. Selective sigma receptor ligands.EBI
Nova Pharmaceutical Corporation
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1.BDB
Max Planck Institute of Molecular Physiology
Hybrid benzothiazole analogs as antiurease agent: Synthesis and molecular docking studies.BDB
Universiti Teknologi MARA (UiTM), Puncak Alam Campus
Evaluation of Natural and Synthetic 1,4-naphthoquinones as Inhibitors of Monoamine Oxidase.BDB
North-West University
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.BDB
University of Karachi
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).BDB
Oregon Health & Science University
Structure and Inhibition of Microbiome -Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.BDB
University of North Carolina at Chapel Hill
Synthesis of benzimidazole derivatives as potent -glucuronidase inhibitors.BDB
Universiti Teknologi MARA (UiTM)
Salicylanilide diethyl phosphates as cholinesterases inhibitors.BDB
Charles University in Prague
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.BDB
Northwestern University