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136 articles for thisTarget

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

Article Title
Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HTEBI
Suven Life Sciences Ltd
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.EBI
Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines.EBI
Warner-Lambert Company
6- and 8-hydroxy-3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans. Dopamine agonists with autoreceptor selectivity.EBI
Warner-Lambert Company
Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analogue of apomorphine.EBI
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.EBI
Neuroleptics from the 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 3. Carboxamidoalkyl derivatives.EBI
Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2.EBI
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.EBI
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.EBI
Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles.EBI
Resolution of 5,6-dihydroxy-2-(N,N-di-n-propylamino)tetralin in relation to the structural and stereochemical requirements for centrally acting dopamine agonists.EBI
1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles.EBI
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.EBI
Design, synthesis, and X-ray data of novel potential antipsychotic agents. Substituted 7-phenylquinolizidines: stereospecific, neuroleptic, and antinociceptive properties.EBI
Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists.EBI
Resolution and absolute configuration of an ergoline-related dopamine agonist, trans-4,4a,5,6,7,8,8a,9-Octahydro-5-propyl-1H(or 2H)-pyrazolo[3,4-g]quinoline.EBI
Preparation of some 10-[3-(dimethylamino)-1-propyl]-10H-pyrazino[2,3-b][1,4] benzothiazines as potential neuroleptics.EBI
Synthesis and central dopaminergic activities of (+/-)-hexahydro-7H-indolo[3,4-gh][1,4]benzoxazine derivatives [(+/-)-9-oxaergolines].EBI
Synthesis of (7R)-7H-indolo[3,4-gh][1,4]benzoxazines, a new class of D-heteroergolines with dopamine agonist activity.EBI
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.EBI
Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain.EBI
Synthesis and dopamine receptor binding of exo- and endo-2-amino-6,7-dihydroxybenzonorbornene, rigid analogues of 2-amino-6,7-dihydroxytetrahydronaphthalene.EBI
Absolute stereochemistry and dopaminergic activity of enantiomers of 2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine.EBI
Synthesis and dopaminergic properties of some exo- and endo-2-aminobenzonorbornenes designed as rigid analogue of dopamine.EBI
2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.EBI
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.EBI
Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.EBI
Aporphines, 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal adenylate cyclase stimulation of 2,10,11-trihydroxyaporphines in comparison with other hydroxylated aporphines.EBI
4a,9b-trans-8-Fluoro-5-(4-fluorophenyl)-2-[4-(4-fluorophenyl)-4-hydroxybutyl]-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole hydrochloride, a new potent neuroleptic.EBI
Conformationally restricted phenothiazine neuroleptics. 1. 3-(Dimethylamino)-1,2,3,4-tetrahydroazepino[3,2,1-kl]phenothiazine.EBI
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.EBI
Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines.EBI
Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines.EBI
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.EBI
Aptuit s.r.l
Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.EBI
Universit£ degli Studi di Chieti Gabriele D'Annunzio
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D3 receptor antagonists.EBI
University of Michigan
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies.EBI
Imperial College
Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization.EBI
Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.EBI
CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist.EBI
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
High-affinity and selective dopamine D3 receptor full agonists.EBI
University of Michigan
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.EBI
Gedeon Richter Plc
Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors.EBI
Harvard Medical School
Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?EBI
Friedrich-Schiller-Universit£t Jena
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-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 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
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.EBI
Universit£ degli Studi di Bari
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.EBI
Universit£ degli Studi di Siena
Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists.EBI
University of Maastricht
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
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
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.EBI
Universita' di Siena
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
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.EBI
University of G£teborg
Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand.EBI
University of Pennsylvania
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
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 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
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.EBI
Synthesis and receptor binding studies relevant to the neuroleptic activities of some 1-methyl-4-piperidylidene-9-substituted-pyrrolo[2,1-b][3]benzazepine derivatives.EBI
Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans.EBI
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
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
Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors.EBI
University of Liège
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
Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity.EBI
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
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 evaluation of 2-aryl- and alkylapomorphines.EBI
University of Debrecen
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
Novel sigma receptor ligands: synthesis and biological profile.EBI
University of Catania
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.EBI
University of Michigan
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
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.EBI
University of Michigan
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.EBI
Lundbeck Research USA, Inc.
Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands.EBI
University of Michigan
Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of dopamine 3 receptor ligands.EBI
University of Michigan
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.EBI
Merck KGaA
Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.EBI
State University of New York
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.EBI
Wake Forest University School of Medicine
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
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.EBI
Università degli Studi di Bari
Antiangiogenic Effect of ()-Haloperidol Metabolite II Valproate Ester [()-MRJF22] in Human Microvascular Retinal Endothelial Cells.EBI
University of Catania
Dopamine D(3) receptor antagonists. 1. Synthesis and structure-activity relationships of 5,6-dimethoxy-N-alkyl- and N-alkylaryl-substituted 2-aminoindans.EBI
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
Novel multifunctional dopamine DEBI
Wayne State University
Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.EBI
University of Siena
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
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
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI
Eli Lilly and Company
Synthesis and optical resolution of (R)- and (S)-trans-7-Hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand.EBI
University of Pennsylvania
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI
Solvay Duphar B.V.
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
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
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.EBI
Huazhong University of Science and Technology
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.EBI
Northeastern University
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.EBI
Azaphenothiazines - promising phenothiazine derivatives. An insight into nomenclature, synthesis, structure elucidation and biological properties.EBI
The Medical University of Silesia
Evaluation of Natural and Synthetic 1,4-naphthoquinones as Inhibitors of Monoamine Oxidase.BDB
North-West University
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).BDB
Oregon Health & Science University