Lipolysis and reesterification: effects of some inhibitors of adenosine 3′,5′-cyclic monophosphate phosphodiesterase

• Main Author: Floyd P. Kupiecki
• Format: Article
• Language: English
• Published: Elsevier 1973-03-01
• Series: Journal of Lipid Research
• Subjects: plasma free fatty acids; 2,3-dihydro-5,6-dimethyl-3-oxo-4-pyridazinecarbonitrile; 2,5-bis(2-chloroethylsulfonyl)-pyrrole-3,4-dicarbonitrile; 2,4-diamino-6-butoxy-s-triazine
• Online Access: http://www.sciencedirect.com/science/article/pii/S0022227520369145

Theophylline and three lipolytic agents, 2,5-bis(2-chloroethylsulfonyl)-pyrrole-3,4-dicarbonitrile (substituted pyrrole),2,4-diamino-6-butoxy-s-triazine (substituted triazine), and 2,3-dihydro-5,6-dimethyl-3-oxo-4-pyridazinecarbonitrile (substituted pyridazine), stimulate basal lipolysis in adipose tissue in vitro. They also cause an increased release of free fatty acids, but not glycerol, from adipose tissue in which lipolysis is already maximally stimulated by epinephrine. The four compounds also inhibit cyclic AMP phosphodiesterase and the conversion of [1-14C]glucose to 14CO2. Evidence is presented that free fatty acids accumulate as the result of inhibited reesterification. The substituted pyridazine and triazine, but not the pyrrole, elevate plasma free fatty acids after oral or intraperitoneal administration in rats.