PMID

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Article Title

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

Universidade Federal De Goi£S

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)

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.

University of Urbino

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.

University of Siena

Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.

Abbott Laboratories

3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).

Hoechst-Roussel Pharmaceuticals

Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.

Smithkline Beecham Pharmaceuticals

(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).

Abbott Laboratories

The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site.

Sandoz Pharma

Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.

Pfizer

 

Serotonin 5-HT₄ agonist activity of a series of meso-azanoradamantane benzamides

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)

Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.

Dipartimento Di Scienze Farmaceutiche

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.

Predix Pharmaceuticals

Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.

University of Kansas

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

Virginia Commonwealth University

Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.

The R. W. Johnson Pharmaceutical Research Institute

alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.

The R. W. Johnson Pharmaceutical Research Institute

Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.

Warner-Lambert

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

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

Isoindolinone enantiomers having affinity for the dopamine D4 receptor.

Parke-Davis Pharmaceutical Research

Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.

Warner-Lambert

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

Solvay Duphar

Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.

Smithkline Beecham Pharmaceuticals

Method of treatment using substituted pyrazolo[1,5-a] pyrimidine compounds

Array Biopharma

Substituted [1,2,4]triazolo[4,3-a]pyrazines as BRD4 inhibitors

Boehringer Ingelheim International

Substituted piperidinyl tetrahydroquinolines

Bayer Pharma Aktiengesellschaft

Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin.

Massachusetts Institute of Technology

Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.

Virginia Commonwealth University

N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.

Nih

Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.

University of Alabama At Birmingham

Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.

Absolute Science

2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.

Tanabe Research Laboratories Usa

Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.

Glaxo Wellcome Research and Development