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
Graphical abstract
1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) attenuated the enhanced glucose excursion following an intraperitoneal glucose tolerance test and the increase in blood pressure in angiotensin-II-induced hypertension in rats. These effects were dose-dependent and well correlated with inhibition of the soluble epoxide hydrolase (sEH) activity in whole blood.
Section snippets
Acknowledgments
Partial support for P.D.J. and B.D.H. came from NIEHS R01 ES002710. B.D.H. is a George and Judy Marcus Senior Fellow of the American Asthma Foundation. P.D.J. was supported in part by an NIH/NHLBI Ruth L. Kirchstein NRSA Grant (F32 HL078096).
References and notes (36)
- A randomized, double-blind, placebo-controlled, dose-ranging, exploratory, 28-day study to examine the effects of...
- et al.
Circ. Res.
(2000) - et al.
Proc. Natl. Acad. Sci.
(2005) - et al.
Life Sci.
(2006)et al.Prostaglandins Other Lipid Mediat.
(2007)et al.Proc. Natl. Acad. Sci. U.S.A.
(2008) - et al.
J. Biol. Chem.
(1993) - et al.
Exp. Physiol.
(2008) - et al.
Arterioscler. Thromb. Vasc. Biol.
(2010) - Chen, D.; Whitcomb, R.; MacIntyre, E.; Tran, V.; Do, Z. N.; Sabry, J.; Patel, D. V.; Anadan, S. K.; Gless, R.; Webb, H....
Curr. Top. Med. Chem.
(2009)Expert Opin. Ther. Patents
(2010)- et al.
Bioorg. Med. Chem. Lett.
(2006)et al.J. Med. Chem.
(2010)
Am. J. Physiol. Cell Physiol.
(2007)
et al.Eur. J. Clin. Invest.
(2006)
et al.Prog. Lipid Res.
(2004)
Obesity
(2010)
et al.J. Pharmacol. Exp. Ther.
(2009)
et al.Diab. Vasc. Dis. Res.
(2008)
et al.J. Pharmacol. Exp. Ther.
(2010)
et al.Exp. Clin. Cardiol.
(2009)
et al.Nat. Rev. Endocrinol.
(2010)
et al.Biochem. Biophys. Res. Commun.
(2005)
(h) Webb, H. WO 08058033 A2,... et al.Trends Pharmacol. Sci.
(2007)
Hypertension
(2005)
Hypertension
(2005)
J. Am. Soc. Nephrol.
(2004)
Am. J. Physiol. Renal Physiol.
(2005)
J. Cardiovasc. Pharmacol.
(2005)
Proc. Natl. Acad. Sci.
(2006)
Cell Biol. Toxicol.
(2009)
Cited by (0)
Copyright © 2010 Elsevier Ltd. All rights reserved.