Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo1,2-cpyrido3,4-epyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

Pamela A Albaugh; Lu Marshall; James GregoryGeoff WhiteAlan HutchisonPhil C. RossDorothy W. CallagherJohn F. TallmanMatt CragoJames V. Cassella

首页> 外文期刊>Journal of Medicinal Chemistry >Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo1,2-cpyrido3,4-epyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

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Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo1,2-cpyrido3,4-epyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

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Benzodiazepines are allosteric modulators of the GABA_A receptor. The traditionally prescribed benzodiazepines are nonselective and suffer from numerous side effects. Upon the identification of receptor subtypes, we set out to discover selective agents with the anticipation that these agents would have superior therapeutic potential. Herein, we describe the synthesis and biological evaluation of substituted 7,8,9,10-tetrahydroimidazo1,2-cpyrido3,4-epyrimidin-5(6H)-ones and disclose that these compounds exhibit functional selectivity at the benzodiazepin receptor of GABA_A receptor subtypes. The α_2/α_3-selective partial agonist 42 exhibited potent in vivo activity.

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《Journal of Medicinal Chemistry》 |2002年第23期|5043-5051|共9页
作者
Pamela A Albaugh; Lu Marshall; James GregoryGeoff WhiteAlan HutchisonPhil C. RossDorothy W. CallagherJohn F. TallmanMatt CragoJames V. Cassella;
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Department of Chemistry, Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405;

Department of Pharmacology, Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405;

Department of Electrophysiology, Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405Department of Molecular Biology, Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405Department of Behavioral Biology, Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405;

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Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo1,2-cpyrido3,4-epyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

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