2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2011 Feb 1;21(3):983-8. doi: 10.1016/j.bmcl.2010.12.042.
Sampath-Kumar Anandan 1,  Heather Kay Webb,  Dawn Chen,  Yi-Xin Jim Wang,  Basker R Aavula,  Sylvaine Cases,  Ying Cheng,  Zung N Do,  Upasana Mehra,  Vinh Tran,  Jon Vincelette,  Joanna Waszczuk,  Kathy White,  Kenneth R Wong,  Le-Ning Zhang,  Paul D Jones,  Bruce D Hammock,  Dinesh V Patel,  Randall Whitcomb,  D Euan MacIntyre,  James Sabry,  Richard Gless
Affiliations

Affiliation

  • 1 Arête Therapeutics, Inc., 7000 Shoreline Court, South San Francisco, CA 94080, United States. anandan30@yahoo.com
PMID: 21211973 DOI: 10.1016/j.bmcl.2010.12.042
Abstract

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.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z