1056675-99-0Relevant articles and documents
1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia
Anandan, Sampath-Kumar,Webb, Heather Kay,Chen, Dawn,Wang, Yi-Xin,Aavula, Basker R.,Cases, Sylvaine,Cheng, Ying,Do, Zung N.,Mehra, Upasana,Tran, Vinh,Vincelette, Jon,Waszczuk, Joanna,White, Kathy,Wong, Kenneth R.,Zhang, Le-Ning,Jones, Paul D.,Hammock, Bruce D.,Patel, Dinesh V.,Whitcomb, Randall,MacIntyre, D. Euan,Sabry, James,Gless, Richard
, p. 983 - 988 (2011/03/20)
1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea 14a (AR9281), a potent and selective soluble epoxide hydrolase inhibitor, was recently tested in a phase 2a clinical setting for its effectiveness in reducing blood pressure and improving insulin resistance in pre-diabetic patients. In a mouse model of diet induced obesity, AR9281 attenuated the enhanced glucose excursion following an intraperitoneal glucose tolerance test. AR9281 also attenuated the increase in blood pressure in angiotensin-II-induced hypertension in rats. These effects were dose-dependent and well correlated with inhibition of the sEH activity in whole blood, consistent with a role of sEH in the observed pharmacology in rodents.
