Effect of cyclonicate, a new hypolipemic drug, on lipolysis in vitro.
A new hypolipemic drug, cyclonicate (3,3,5-trimethyl-cyclohexyl nicotinate), was studied and its effects were compared with those of nicotinic acid. Experiments were carried out in vitro on rat adipose tissue on spontaneous lipolysis, and on lipolysis stimulated by noradrenaline, theophylline, dibutyryl cyclic AMP. Cyclonicate, like nicotinic acid, reduced the lipolytic stimulation of theophylline. Its effect was dose-dependent but 10 times lower (IC50 = 1 mM) than that of nicotinic acid. The inhibitory activity of both compounds was higher on theophylline-induced lipolysis than on noradrenaline-stimulated lipolysis. Neither one had any effect on dibutyryl cyclic AMP. In the absence of stimulating drugs, cyclonicate increased the FFA/glycerol ratio, more than nicotinic acid. Moreover, cyclonicate inhibited theophylline-induced FFA release much less than glycerol release, while under the same conditions, nicotinic acid inhibited both FFA and glycerol release. Thus cyclonicate would influence not only triglyceride hydrolysis, but also FFA utilization by adipose tissue.
D000273:Adipose Tissue / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D000242:Cyclic AMP / Q000494:pharmacology; D005230:Fatty Acids, Nonesterified / Q000378:metabolism; D005990:Glycerol / Q000378:metabolism; D000960:Hypolipidemic Agents / Q000494:pharmacology*; D066298:In Vitro Techniques; D008066:Lipolysis / Q000187:drug effects*; D008297:Male; D009525:Niacin; D009539:Nicotinic Acids / Q000494:pharmacology*; D009638:Norepinephrine / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013806:Theophylline / Q000494:pharmacology
D005230:Fatty Acids, Nonesterified; D000960:Hypolipidemic Agents; D009539:Nicotinic Acids; D009525:Niacin; C032821:ciclonicate; D013806:Theophylline; D000242:Cyclic AMP; D005990:Glycerol; D009638:Norepinephrine