Antilipolytic activity of viprostol, a transdermally active antihypertensive PGE2 analog.
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.
D015056:1-Methyl-3-isobutylxanthine / Q000494:pharmacology; D000273:Adipose Tissue / Q000187:drug effects / Q000378:metabolism*; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D015232:Dinoprostone / Q000031:analogs & derivatives*; D004837:Epinephrine / Q000494:pharmacology; D005990:Glycerol / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008066:Lipolysis / Q000187:drug effects*; D008297:Male; D009765:Obesity / Q000378:metabolism*; D011459:Prostaglandins E, Synthetic / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D000959:Antihypertensive Agents; D011459:Prostaglandins E, Synthetic; D015232:Dinoprostone; C034232:viprostol; D005990:Glycerol; D015056:1-Methyl-3-isobutylxanthine; D004837:Epinephrine