Antilipolytic activity of viprostol, a transdermally active antihypertensive PGE2 analog

Autor: David L. Crandall, Barbara A. Davis, Peter Cervoni, Florence H. Lizzo, Vanessa Vu
Rok vydání: 1987
Předmět:
Zdroj: Prostaglandins. 33:767-773
ISSN: 0090-6980
DOI: 10.1016/0090-6980(87)90042-6
Popis: Viprostol, a novel prostaglandin E2 congener, was assessed for in vitro antilipolytic activity in the spontaneously obese rat. In isolated epididymal adipocytes, viprostol exhibited a dose-dependent inhibition of catecholamine-stimulated lipolysis at concentrations ranging from 10 microM to 1 mM, but was ineffective at lower concentrations. Additionally, viprostol exhibited approximately 50% of the antilipolytic activity of naturally-occurring PGE1 and PGE2 at similar concentrations, but was as potent as PGF2 alpha. At 10 microM, viprostol inhibited maximum catecholamine-stimulated lipolysis by approximately 35% of the total, hormone-stimulated glycerol release. The results of these experiments indicate that viprostol exhibits antilipolytic activity in vitro, but is less potent than the naturally-occurring PGE's to which it is most closely related structurally.
Databáze: OpenAIRE