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 Jim; 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

Anandan, Sampath-Kumar; Webb, Heather Kay; Chen, Dawn; Wang, Yi-Xin Jim; 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.

Affiliation

Anandan SK; Arête Therapeutics, Inc., 7000 Shoreline Court, South San Francisco, CA 94080, United States. anandan30@yahoo.com

Bioorg Med Chem Lett ; 21(3): 983-8, 2011 Feb 01.

Article in En | MEDLINE | ID: mdl-21211973

Subject(s)

Adamantane/analogs & derivatives; Antihypertensive Agents/chemistry; Enzyme Inhibitors/chemistry; Epoxide Hydrolases/antagonists & inhibitors; Hypertension/drug therapy; Insulin Resistance; Urea/analogs & derivatives; Adamantane/chemistry; Adamantane/pharmacokinetics; Adamantane/therapeutic use; Administration, Oral; Angiotensin II/pharmacology; Animals; Antihypertensive Agents/pharmacokinetics; Antihypertensive Agents/therapeutic use; Blood Glucose/analysis; Disease Models, Animal; Enzyme Inhibitors/pharmacokinetics; Enzyme Inhibitors/therapeutic use; Epoxide Hydrolases/metabolism; Hypertension/chemically induced; Mice; Obesity/drug therapy; Rats; Urea/chemistry; Urea/pharmacokinetics; Urea/therapeutic use

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Full text: 1 Database: MEDLINE Main subject: Urea / Insulin Resistance / Adamantane / Enzyme Inhibitors / Epoxide Hydrolases / Hypertension / Antihypertensive Agents Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Type: Article Affiliation country: United States

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