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Vol. 59, Issue 2, 349-357, February 2001

Characterization of a G Protein-Coupled Receptor for Nicotinic Acid

Anna Lorenzen, Christina Stannek, Heidrun Lang, Viktor Andrianov, Ivars Kalvinsh, and Ulrich Schwabe

Institute of Pharmacology, University of Heidelberg, Heidelberg, Germany (A.L., C.S., H.L., U.S.); and Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Riga, Latvia (V.A., I.K.)

Nicotinic acid is a lipid-lowering agent widely used to treat hypertriglyceridemia and to elevate low high density lipoprotein levels. However, the underlying mechanisms are poorly understood. In this study, G protein activation by nicotinic acid and derivatives was assessed as stimulation of guanosine 5'-(gamma -[35S]-thio)triphosphate ([35S]GTPgamma S) binding, and [3H]nicotinic acid was used for specific labeling of binding sites. Nicotinic acid (EC50 ~1 µM) stimulated [35S]GTPgamma S binding in membranes from rat adipocytes and spleen, but not from other tissues. G protein activation in adipocyte membranes in the presence of maximally activating concentrations of the selective A1 adenosine receptor agonist 2-chloro-N6-cyclopentyladenosine and nicotinic acid was almost additive, indicating that G proteins of mostly distinct pools were activated by these agonists. G protein activation by nicotinic acid and related substances in spleen and adipocytes revealed identical pharmacological profiles. [3H]Nicotinic acid specifically detected guanine nucleotide-sensitive binding sites of identical pharmacology in adipocyte and spleen membranes. The site of action of nicotinic acid is distinct from other G protein-coupled receptors. These data indicate that nicotinic acid most probably acts on a specific G protein-coupled receptor.

Copyright © 2001 by The American Society for Pharmacology and Experimental Therapeutics


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