PMID

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Article Title

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Three-dimensional quantitative structure-activity relationships of 5-HT receptor binding data for tetrahydropyridinylindole derivatives: a comparison of the Hansch and CoMFA methods.

University Of Georgia

(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.

Smithkline Beecham Pharmaceuticals

2,3-Dihydrobenzofuran analogues of hallucinogenic phenethylamines.

Purdue University

Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes.

Mitsubishi Kasei

A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors.

Virginia Commonwealth University

6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists.

Eli Lilly

Ergolines as selective 5-HT1 agonists.

Eli Lilly

Synthesis and serotonin receptor affinities of a series of enantiomers of alpha-methyltryptamines: evidence for the binding conformation of tryptamines at serotonin 5-HT1B receptors.

Purdue University

N-methyl derivatives of the 5-HT2 agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.

TBA

Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.

TBA

5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues.

TBA

2,3-Dialkyl(dimethylamino)indoles: interaction with 5HT1, 5HT2, and rat stomach fundal serotonin receptors.

TBA

5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.

TBA

New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.

Meiji Seika Kaisha

Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.

Huazhong University Of Science And Technology

Steric structure-activity relationship of cyproheptadine derivatives as inhibitors of histone methyltransferase Set7/9.

Tokyo Medical And Dental University (Tmdu)

5-HT2 receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives.

Medical University Of Warsaw

Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.

Dipartimento Di Farmacia Universit£

The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.

Gedeon Richter

Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.

Huazhong University Of Science And Technology

Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential.

Iqm-Csic

Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent.

Jagiellonian University Medical College

Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT1A receptor functional profile.

Jagiellonian University Medical College

Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.

Universit£

Identification of a new selective dopamine D4 receptor ligand.

Florida A&M University

Synthesis and biological evaluation of a series of benzoxazole/benzothiazole-containing 2,3-dihydrobenzo[b][1,4]dioxine derivatives as potential antidepressants.

Huazhong University Of Science And Technology

Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.

Universidade Federal De Goi£S

Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.

Merck Sharp & 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.

Merrell Dow Research Institute

 

Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine.

TBA

Application of desirability-based multi(bi)-objective optimization in the design of selective arylpiperazine derivates for the 5-HT1A serotonin receptor.

University Of Porto

Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.

Eli Lilly

Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.

Merck Sharp & Dohme Research Laboratories

Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.

Merck Sharp And Dohme Research Laboratories

New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.

University Of Santiago

Discovery and SAR of org 24598-a selective glycine uptake inhibitor.

Organon Research And Development Group

Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.

Universidad De Santiago De Compostela

 

Synthesis, biological in vitro evaluation and stereoselectivity of ondansetron analogues: novel 5-HT2A receptor antagonists

TBA

Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents.

Sk Biopharmaceuticals

Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1.

Medical University Of Warsaw

Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.

Aska Pharmaceutical

Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.

Universidade Federal Do Rio Grande Do Sul

Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.

European Research Centre For Drug Discovery And Development (Natsyndrugs)

Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands.

Jagiellonian University Medical College

The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones.

Jagiellonian University Medical College

Activity of Parthenolide at 5HT2A receptors.

University Of Montana

Total synthesis and evaluation of [18F]MHMZ.

University Of Mainz

7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands.

Jagiellonian University Medical College

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.

Brigham & Women'S Hospital

Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.

Faes Farma

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.

H. Lundbeck

A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.

Alcon Research

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.

Universit£

4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.

Merck Sharp And Dohme Research Laboratories

Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.

Universit£

Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).

Purdue University

Current and novel approaches to the drug treatment of schizophrenia.

Merck Sharp And Dohme Research Laboratories

Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.

Universit£

Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.

Universit£

(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.

Astra Arcus

Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.

Universit£

Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.

Universit£

Ketanserin analogues: the effect of structural modification on 5-HT2 serotonin receptor binding.

Virginia Commonwealth University

Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.

Vanderbilt University

Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.

Universit£

Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.

H. Lundbeck

18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.

University Of Pennsylvania

Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans.

H. Lundbeck

SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.

Searle Research And Development

Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.

Virginia Commonwealth University

Pyrrole mannich bases as potential antipsychotic agents.

R. W. Johnson Pharmaceutical Research Institute

Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.

Virginia Commonwealth University

Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.

Bristol-Myers Squibb

Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.

Centre De Recherches De Vitry Alfortville Rh£Ne-Poulenc Rorer

Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.

Hoechst-Roussel Pharmaceuticals

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.

Dainippon Pharmaceutical

Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.

Abbott Laboratories

Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.

Warner-Lambert

Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors.

Eli Lilly

The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.

Bristol-Myers

Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.

H. Lundbeck

Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.

TBA

2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.

Duphar Research Laboratories

Antipsychotic activity of substituted gamma-carbolines.

Wyeth Laboratories

Central serotonin receptors as targets for drug research.

TBA

Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives.

TBA

Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.

TBA

N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists.

Welfide

Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.

Yale University

 

1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists

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.

Universit£

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.

Jagiellonian University Medical College

New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation.

Universit£

New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage.

Universidad Complutense De Madrid

Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands.

Jagiellonian University Medical College

Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.

Universit£

Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.

Arena Pharmaceuticals

Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.

Universita Di Siena

Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581.

Universidade Federal De Goi£S

New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation.

Universit£

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.

Jagiellonian University Medical College

Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.

Pfizer

Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives.

Jagiellonian University Medical College

Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.

Universit£

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.

TBA

 

Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity.

TBA

 

5-HT_1A and 5-HT_2A ligands with anxiolytic and antipanic-like properties

TBA

 

4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT_2A receptor antagonists

TBA

 

2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT_1A receptor ligand

TBA

 

Synthesis and serotonin receptor binding properties of 5-substituted 3-(1′,2′,5′,6′-tetrahydropyridin-3′-yl) indoles

TBA

 

Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents

TBA

Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.

European Research Centre For Drug Discovery And Development (Natsyndrugs)

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.

Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz

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.

University Of Siena

Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.

Università

'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines.

University Of Wisconsin-La Crosse

The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.

Purdue University

Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.

Pfizer

1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems.

Università

R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.

Harvard Medical School

Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.

Alcon Research

Novel sigma receptor ligands: synthesis and biological profile.

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.

University Of Montpellier

Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors.

Faculté

Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.

Université

Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines.

Central Drug Research Institute

Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.

Merck Sharp And Dohme Research Laboratories

1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.

Purdue University

C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.

Purdue University

1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.

Alcon Research

New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.

Università

SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.

Organix

4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.

Merck Sharp And Dohme Research Laboratories

Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.

Università

Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.

Università

Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.

Virginia Commonwealth University

Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.

Merck

New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.

Collegium Medicum Of The Jagiellonian University

Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.

Virginia Commonwealth University

Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.

Virginia Commonwealth University

Binding of beta-carbolines at 5-HT(2) serotonin receptors.

Virginia Commonwealth University

Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.

Virginia Commonwealth University

Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.

Purdue University

Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor.

Virginia Commonwealth University

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.

Universidad Complutense

Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.

Università

Development of a presynaptic 5-HT1A antagonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.

University Of LièGe

Translocation of the 5-alkoxy substituent of 2,5-dialkoxyarylalkylamines to the 6-position: effects on 5-HT(2A/2C) receptor affinity.

Purdue 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.

University Center For Pharmacy

Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.

Université

Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.

Virginia Commonwealth University

N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.

Merck Sharp & Dohme Research Laboratories

1-[2-methoxy-5-(3-phenylpropyl)]-2-aminopropane unexpectedly shows 5-HT(2A) serotonin receptor affinity and antagonist character.

Virginia Commonwealth University

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.

Universidad De Navarra

Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity.

Polish Academy Of Sciences

Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT(2A/2C) receptor agonists.

Purdue University

A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties.

Purdue University

Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.

Virginia Commonwealth University

Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines.

Purdue University

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

Virginia Commonwealth University

1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists.

Virginia Commonwealth University

Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor.

Astrazeneca R&D SöDertäLje

Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists.

Jagiellonian University

N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.

Yoshitomi Pharmaceutical Industries

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.

Virginia Commonwealth University

Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain.

Purdue University

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.

Knoll Pharmaceuticals

New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.

University Of GöTeborg

N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.

Postech

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.

Recordati

Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and alpha1 receptor binding affinity.

Angelini Ricerche

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).

Centro De InvestigacióN Grupo Ferrer

NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.

Neurogen

Serotonergic ergoline derivatives.

Pharmacia & Upjohn

Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.

R. W. Johnson Pharmaceutical Research Institute

A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.

Purdue University

Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding.

Virginia Commonwealth University

Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity.

Purdue University

Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.

University Of Groningen

Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives.

Purdue University

Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.

Warner-Lambert

[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.

Università

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.

Universidad Complutense

Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole.

H. Lundbeck

Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups.

Purdue University

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.

Yamanouchi Pharmaceutical

3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.

Pfizer

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.

Hoechst-Roussel Pharmaceuticals

(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.

Wyeth Research (Uk)

Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.

Virginia Commonwealth University

Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar

New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.

University Of LièGe

Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.

Vanderbilt University

Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.

Hoechst-Roussel Pharmaceuticals

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.

Scios Nova

Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes.

Purdue University

Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.

H. Lundbeck

Synthesis and evaluation of a novel series of N,N-dimethylisotryptamines.

TBA

In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.

TBA

N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin.

Virginia Commonwealth University

Serotonergic properties of spiroxatrine enantiomers.

University Of Arizona

2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.

Duphar Research Laboratories

Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.

Warner-Lambert

(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.

TBA

Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.

Mcneil Pharmaceutical And Janssen Research Foundation Worldwide

2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors.

Ciba-Geigy

3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.

Pfizer

5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.

Virginia Commonwealth University

Binding of indolylalkylamines at 5-HT2 serotonin receptors: examination of a hydrophobic binding region.

Virginia Commonwealth University

Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.

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.

H. Lundbeck

Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.

Virginia Commonwealth University

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.

Abbott Laboratories

Benzofuran bioisosteres of hallucinogenic tryptamines.

Purdue University

Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.

University Of Pennsylvania

Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.

Pfizer

1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors.

Pfizer

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.

Hoechst-Roussel Pharmaceuticals

Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.

H. Lundbeck

Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.

H. Lundbeck

Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.

H. Lundbeck

One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.

University Of Karachi

Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).

Oregon Health & Science University

Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.

University Of Wisconsin-Madison

Synthesis, biological evaluation and molecular docking of N-phenyl thiosemicarbazones as urease inhibitors.

University Of Karachi

Salicylanilide diethyl phosphates as cholinesterases inhibitors.

Charles University In Prague

Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study.

Swiss Federal Institute Of Technology