Imidazo[1,2-a]pyridines: Orally Active Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor
详细信息 查看全文
- 作者：Andr茅s A. Trabanco ; Gary Tresadern ; Gregor J. Macdonald ; Juan Antonio Vega ; Ana Isabel de Lucas ; Encarnaci贸n Matesanz ; Ar谩nzazu Garc铆a ; Mar铆a Lourdes Linares ; Sergio A. Alonso de Diego ; Jos茅 Manuel Alonso ; Daniel Oehlrich ; Abdelah Ahnaou ; Wilhelmus Drinkenburg ; Claire Mackie ; Jos茅 Ignacio Andr茅s ; Hilde Lavreysen ; Jos茅 Mar铆a Cid
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：March 22, 2012
- 年：2012
- 卷：55
- 期：6
- 页码：2688-2701
- 全文大小：548K
- 年卷期：v.55,no.6(March 22, 2012)
- ISSN：1520-4804
文摘
Advanced leads of an imidazopyridine series of positive allosteric modulators of the metabotropic glutamate 2 (mGlu2) receptor are reported. The optimization of in vitro ADMET and in vivo pharmacokinetic properties led to the identification of 27o. With good potency and selectivity for the mGlu2 receptor, 27o affected sleep鈥搘ake architecture in rats after oral treatment, which we have previously shown to be indicative of mGlu2 receptor-mediated central activity.