Journal of Medicinal Chemistry p. 220 - 240 (2013)
Update date:2022-08-15
Topics:
Plowright, Alleyn T.
Nilsson, Karolina
Antonsson, Madeleine
Amin, Kosrat
Broddefalk, Johan
Jensen, J?rgen
Lehmann, Anders
Jin, Shujuan
St-Onge, Stephane
Tomaszewski, Miros?aw J.
Tremblay, Maxime
Walpole, Christopher
Wei, Zhongyong
Yang, Hua
Ulander, Johan
Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic effects, it has been suggested that the CB1 receptors in the periphery could play a significant role in reducing reflux. A moderately potent and highly lipophilic series of 2-aminobenzamides was identified through focused screening of GPCR libraries. Development of this series focused on improving potency and efficacy at the CB1 receptor, reducing lipophilicity and limiting the central nervous system (CNS) exposure while maintaining good oral absorption. Improvement of the series led to compounds having excellent potency at the CB1 receptor and high levels of agonism, good physical and pharmacokinetic properties, and low penetration into the CNS. A range of compounds demonstrated a dose-dependent inhibition of transient lower esophageal sphincter relaxations in a dog model.
View MoreContact:410-273-7300; 800-221-3953
Address:4609 Richlynn Dr., PO Box 369, Belcamp, MD, 21017-0369, USA
NingBO Hong Xiang Biochem.Co.Ltd
website:http://www.hxbiochem.com
Contact:0574-66003444
Address:Ning Bo Bei Lun
Hangzhou Share Chemical Co., Ltd(expird)
Contact:+86-57187093700
Address:Hang Xing Road
TAIZHOU XINGCHENG CHEMPHARM CO.,LTD.
Contact:0086-0576-88551200,88886292 ,88880039
Address:B Area. 10 Floor.Yaodadasha. 289#.Shifu Road.Taizhou.Zhejiang.China
YanCheng LongShen Chemical Co.,Ltd.
Contact:+86-515-86668866
Address:No.13,Weiyi Road,Funing Aoyang Industrial Park
Doi:10.1016/j.bmcl.2009.11.089
(2010)Doi:10.1002/asia.201100392
(2011)Doi:10.1002/pola.25042
(2012)Doi:10.1016/S0040-4039(00)80562-6
(1988)Doi:10.1016/j.carres.2006.10.009
(2007)Doi:10.1021/jacs.0c11448
(2021)