Forskolin an an activator of cyclic AMP accumulation and lipolysis in rat adipocytes

I. Litosch, T. H. Hudson, I. Mills, J. N. Fain

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108 Scopus citations

Abstract

Forskolin increased cyclic AMP accumulation in isolated adipocytes and markedley potentiated the elevation of cyclic AMP due to isoproterenol. In adipocyte membranes, forskolin stimulated adenylate cyclase activity at concentrations of 0.1 μM or greater. Forskolin did not affect the EC50 for activation of adenylate cyclase but did increase the maximal effect of isoproterenol. Neither the soluble nor particulate low-K(m) cyclic AMP phosphodiesterase activity was affected by forskolin. Low concentrations of forskolin (0.1-1.0 μM), which significantly elevated cyclic AMP levels, did not increase lipolysis, whereas similar increases in cyclic AMP levels due to isoproterenol elevated lipolysis. Forskolin did not inhibit the activation of triacylglycerol lipase by cyclic AMP-dependent protein kinase or the subsequent hydrolysis of triacylglycerol. Higher concentrations of forskolin (10-100 μM) did increase lipolysis. Both the increased cyclic AMP production and lipolysis due to forskolin were inhibited by the antilipolytic agents insulin and N6-(phenylisopropyl)adenosine. Hypothyroidism reduced the ability of forskolin to stimulate cyclic AMP production and lipolysis. These results indicate that forskolin increases cyclic AMP production in adipocytes through an activation of adenylate cyclase. Lipolysis is activated by forskolin but at higher concentrations of total cyclic AMP than for catecholamines.

Original languageEnglish (US)
Pages (from-to)109-115
Number of pages7
JournalMolecular Pharmacology
Volume22
Issue number1
StatePublished - Oct 5 1982

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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    Litosch, I., Hudson, T. H., Mills, I., & Fain, J. N. (1982). Forskolin an an activator of cyclic AMP accumulation and lipolysis in rat adipocytes. Molecular Pharmacology, 22(1), 109-115.