Human Beta3 Adrenergic Receptor Agonists Containing Imidazolidinone and Imidazolone Benzenesulfonamides

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Apr 14

PMID 10201842

Citations 2

Authors

E M Naylor

E R Parmee

V J Colandrea

L Perkins

L Brockunier

M R Candelore

M A Cascieri

L F Colwell Jr

L Deng

W P Feeney

M J Forrest

G J Hom

D E Macintyre

C D Strader

L Tota

P R Wang

M J Wyvratt

M H Fisher

A E Weber

Affiliations

Soon will be listed here.

Abstract

The cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.

Citing Articles

Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.

Kumar P, Bharatam P Med Chem Res. 2010; 19(9):1121-1140.

PMID: 21170122 PMC: 2988205. DOI: 10.1007/s00044-009-9257-x.

Prototropic tautomerism of imidazolone in aqueous solution: a density functional approach using the combined discrete/self-consistent reaction field (SCRF) models.

Ren Y, Li M, Wong N J Mol Model. 2005; 11(2):167-73.

PMID: 15744506 DOI: 10.1007/s00894-005-0242-0.