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 MoreHangzhou Hysen Pharma co.,Ltd.
website:http://www.hysenpharma.cn/
Contact:0086-571-88298791
Address:#701,Gudun Road Hangzhou
Shandong Dayi Chemical Co., Ltd.
website:http://www.dayi.com.cn
Contact:+86- 535-7388728. 15306386031
Address:No 1 Danya west road, Laiyang City, Shandong province
wuxi huabin bio-tech Co.,Ltd(expird)
Contact:86-0510-85133006
Address:hubin road NO157
Tianjin Derchemist Sci-Tech Co., Ltd.
website:http://www.derchemist.com
Contact:+86-22-58627059
Address:Xinmao Science and Technology Park,Huayuan Industrial Park
Zhejiang Allied Chemical Co.,Ltd
Contact:18967038207
Address:Area A-30, High-tech Industrial Park, Quzhou, Zhejiang, China.
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)