Search Results - "Wright, Jon L"
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3-Arylimino-2-indolones Are Potent and Selective Galanin GAL3 Receptor Antagonists
Published in Journal of medicinal chemistry (29-06-2006)“…A series of 3-imino-2-indolones are the first published, high-affinity antagonists of the galanin GAL3 receptor. One example,…”
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Subtype-Selective N-Methyl-d-Aspartate Receptor Antagonists: Synthesis and Biological Evaluation of 1-(Heteroarylalkynyl)-4-benzylpiperidines
Published in Journal of medicinal chemistry (07-09-2000)“…4-[4-(4-Benzylpiperidin-1-yl)but-1-ynyl]phenol (8) and 4-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]phenol (9) are potent NR1a/2B receptor antagonists (IC50 values…”
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The Discovery and Structure-Activity Relationships of 1,2,3,6-Tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine Autoreceptor Agonists and Potential Antipsychotic Agents
Published in Journal of medicinal chemistry (01-10-1994)“…A novel dopamine (DA) autoreceptor agonist, 1,2,3,6-tetrahydro-4-phenyl-1- [(3-phenyl-3-cyclohexen-1-yl)methyl]pyridine (14), was identified. The…”
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Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues
Published in Bioorganic & medicinal chemistry letters (08-03-2004)“…A benzylpiperidine analogue with an acetylenic linker, 5-(3-[4-(4-fluorobenzyl)-piperidin-1-yl]-prop-1-ynyl)-1,3-dihydrobenzimidazol-2-one (3), was identified…”
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Synthesis of N-Substituted 4-(4-Hydroxyphenyl)piperidines, 4-(4-Hydroxybenzyl)piperidines, and (±)-3-(4-Hydroxyphenyl)pyrrolidines: Selective Antagonists at the 1a/2B NMDA Receptor Subtype
Published in Journal of medicinal chemistry (09-03-2000)“…Antagonists at the 1a/2B subtype of the NMDA receptor (NR1a/2B) are typically small molecules that consist of a 4-benzyl- or a 4-phenylpiperidine with an…”
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Discovery of selective dopamine D4 receptor antagonists: 1-Aryloxy-3-(4-aryloxypiperidinyl)-2-propanols
Published in Bioorganic & medicinal chemistry letters (03-06-1997)“…High volume screening identified 3-(4-benzylpiperidinyl)-1-naphthoxy-2-propanol as a selective dopamine D4 receptor ligand. A systematic structure-activity…”
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Subtype-Selective N-Methyl-d-aspartate Receptor Antagonists: Synthesis and Biological Evaluation of 1-(Arylalkynyl)-4-benzylpiperidines
Published in Journal of medicinal chemistry (01-07-1999)“…A search of our compound library for compounds with structural similarity to ifenprodil (5) and haloperidol (7) followed by in vitro screening revealed that…”
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Identification, Characterization and Pharmacological Profile of Three Metabolites of (R)-(+)-1,2,3,6-Tetrahydro-4-phenyl-1-[(3-phenylcyclohexen-1-yl)methyl]p yridine (CI-1007), a Dopamine Autoreceptor Agonist and Potential Antipsychotic Agent
Published in Journal of medicinal chemistry (01-12-1995)Get full text
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3-Arylimino-2-indolones Are Potent and Selective Galanin GAL 3 Receptor Antagonists
Published in Journal of medicinal chemistry (01-06-2006)Get full text
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3-arylimino-2-indolones are potent and selective galanin GAL3receptor antagonists
Published in Journal of medicinal chemistry (2006)Get full text
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Discovery of subtype-selective NMDA receptor ligands : 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists
Published in Bioorganic & medicinal chemistry letters (04-10-1999)“…4-Benzyl-1-[4-(1H-imidazol-4-yl)but-3-ynyl]piperidine (8) has been identified as a potent antagonist of the NR1A/2B subtype of the NMDA receptor. When dosed…”
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Parallel synthesis of a series of subtype-selective NMDA receptor antagonists
Published in Bioorganic & medicinal chemistry letters (20-03-2000)“…A series of 1-(heteroarylthioalkyl)-4-benzylpiperidines was rapidly synthesized through the use of parallel synthesis to investigate the binding affinity for…”
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Pharmacological Characterization of PD 152255, a Novel Dimeric Benzimidazole Dopamine D 3 Antagonist
Published in Pharmacology, biochemistry and behavior (01-02-1998)“…152255 ( E-1, 1′-(2-butene-1,4-diyl)bis [2-[4-[3-(1-piperidinyl)propoxy]-phenyl]-1H-benzimidazole]) exhibited high affinity ( K i = 12.7 nM) for human dopamine…”
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Pharmacological characterization of PD 152255, a novel dimeric benzimidazole dopamine D3 antagonist
Published in Pharmacology, biochemistry and behavior (01-02-1998)“…152255 (E-1,1'-(2-butene-1,4-diyl)bis[2-[4-[3-(1-piperidinyl)propoxy]-phe nyl]-1H-benzimidazole]) exhibited high affinity (Ki = 12.7 nM) for human dopamine…”
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4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2-naphthalenecarboxamides: Selective dopamine D 3 receptor partial agonists
Published in Bioorganic & medicinal chemistry letters (18-06-1996)“…A series of 4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2-naphthalenecarboxamide dopamine (DA) D 3 receptor agonists has been identified. These…”
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Discovery of subtype-selective NMDA receptor ligands: 4-Benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1 a/2B antagonists
Published in Bioorganic & medicinal chemistry letters (1999)“…4-Benzyl-1-[4-(1 H -imidazol-4-yl)but-3-ynyl]piperidine ( 8) has been identified as a potent antagonist of the NR1 a/2B subtype of the NMDA receptor. When…”
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