PMID

Data

Article Title

Organization

Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.

University of Illinois At Chicago

The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.

Virginia Commonwealth University

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

 

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

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

Novel azulene derivatives for the treatment of erectile dysfunction.

Friedrich-Alexander University

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

Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.

Clinic of Nuclear Medicine

Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.

Friedrich-Alexander University

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

2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.

Laboratoire De Chimie Th�Rapeutique

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.

Universit£

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

2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.

Friedrich-Alexander University

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

Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding.

Forschungszentrum J£Lich

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£

Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands.

University of Santiago De Compostela

Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET.

Friedrich-Alexander-UniversitäT Erlangen-NüRnberg

Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.

Friedrich-Alexander University

Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.

Friedrich-Alexander University

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£

1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.

Friedrich-Alexander University

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

 

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 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

?-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.

Univ. Grenoble Alpes

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

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.

Beijing Normal University

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

Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.

Cracow University of Technology

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

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

Synthesis and biological investigation of new equatorial (?) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.

Medical University of Warsaw

Isoquinolinone derivatives as potent CNS multi-receptor D

Jiangsu Ocean University

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

The Essential Medicinal Chemistry of Cannabidiol (CBD).

University of Minnesota

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

Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.

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.

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

Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.

Usona Institute

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

Virginia Commonwealth University

Benzimidazolone-based selective ?

University of Florida

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

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

Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.

Cracow University of Technology

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

Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.

Jagiellonian University Medical College

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

Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.

Cracow University of Technology

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

Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.

University of Maryland

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

Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.

Universidade Federal Do Rio De Janeiro

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

Hoechst-Roussel Pharmaceuticals

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

Two new phenylpiperazines with atypical antipsychotic potential.

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.

Central Drug Research Institute

Multistructure 3D-QSAR studies on a series of conformationally constrained butyrophenones docked into a new homology model of the 5-HT2A receptor.

Universitat Pompeu Fabra

Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.

Pierre Fabre Research Center

GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.

University of Perugia

Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.

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.

Universidad De Santiago

New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.

Faes

A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.

Monash University

(+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity.

Sandoz Pharma

Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.

University of Santiago De Compostela

Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.

Huazhong University of Science and Technology

New 5-HT

Dipartimento Di Farmacia Universit£

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

Bristol-Myers Squibb Pharmaceutical Research Institute

 

Synthesis and pharmacological evaluation of 4-[2- hydroxy-3-(4-phenyl-piperazin-1-yl)-propoxy]-4- azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

The Medical University of Warsaw

Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.

Case Western Reserve University

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.

Kyowa Hakko Kogyo

Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines.

Harvard University

Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.

Case Western Reserve University

3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.

Case Western Reserve University

The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways.

Institut De Recherches Servier

L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.

Case Western Reserve University

Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.

Case Western Reserve University

Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles: new selective ligands of the 5-HT(7) receptor.

Meiji Seika Kaisha

The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist.

Astrazeneca R&D

The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.

Case Western Reserve University

Investigations into migraine pathogenesis: time course for effects of m-CPP, BW723C86 or glyceryl trinitrate on appearance of Fos-like immunoreactivity in rat trigeminal nucleus caudalis (TNC).

Roche Bioscience

Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications.

Nih

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.

Centre De Recherches De Croissy

Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.

Institut De Recherches Servier

Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.

TBA

Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.

Sri International

Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.

University of Toronto

Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.

H. Lundbeck

Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.

Emory University

The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.

Preclinical R & D, Astra Arcus

RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.

Roche Bioscience

BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.

Smithkline Beecham Pharmaceuticals

PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties.

Pharmacia & Upjohn

Iloperidone binding to human and rat dopamine and 5-HT receptors.

Hoechst Marion Roussel

Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.

SynthÉLabo Recherche

Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist.

Pharmacia and Upjohn

Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.

Janssen Research Foundation

A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.

Abbott Laboratories

Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor.

University of Turku

Radioreceptor binding profile of the atypical antipsychotic olanzapine.

Eli Lilly

GR127935: a potent and selective 5-HT1D receptor antagonist.

Glaxo Research and Development

Novel discriminatory ligands for 5-HT2B receptors.

Smithkline Beecham Pharmaceuticals

Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.

Smithkline Beecham Pharmaceuticals

BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex.

Boehringer Ingelheim Italia

Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.

Vrije Universiteit

Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo.

Syntex Discovery Research

D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs.

Case Western Reserve University

Species differences in the pharmacology of the 5-hydroxytryptamine2 receptor: structurally specific differentiation by ergolines and tryptamines.

Eli Lilly

Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist.

Fujisawa Pharmaceutical

Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists.

Institut De Recherches Servier

Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties.

Dainippon Pharmaceutical

Molecular biology of 5-HT receptors.

University of Alberta

Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.

Yamanouchi Pharmaceutical

Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.

Case Western Reserve University

PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor.

Karolinska Institutet

The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors.

Syntex Discovery Research

Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity.

Eli Lilly

Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity.

Janssen Research Foundation

(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.

Abbott Laboratories

pH-dependent modulation of agonist interactions with [3H]-ketanserin-labelled S2 serotonin receptors.

University of Toronto

Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers.

Organon International

Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity.

Schering-Plough

McN-5652: a highly potent inhibitor of serotonin uptake.

Mcneil Pharmaceutical

1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.

The Oregon Health Sciences University

Effects of remoxipride and some related new substituted salicylamides on rat brain receptors.

Astra LÄKemedel

Differentiation of 5-hydroxytryptamine2 receptor subtypes using 125I-R-(-)2,5-dimethoxy-4-iodo-phenylisopropylamine and 3H-ketanserin.

Stanford University

Binding of arylpiperazines to 5-HT3 serotonin receptors: results of a structure-affinity study.

Virginia Commonwealth University

Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotonin.

Lundbeck Ais

[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.

Nida Addiction Research Center

The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.

Novo Industri

Neurochemical profile of eltoprazine.

Duphar

Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors.

Eli Lilly

Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.

Center For Bio-Pharmaceutical Sciences

SDZ 205-557, a selective, surmountable antagonist for 5-HT4 receptors in the isolated guinea pig ileum.

Sandoz Pharma

Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist.

Sanofi Recherche

NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.

Novo Nordisk

Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist.

University of North Carolina

Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors.

Stanford University

Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.

Universita Degli Studi Di Bari