Alteration of alpha and muscarinic receptors in rat brain and heart following chronic nicotine treatment.

Adrenergic and muscarinic binding sites in 4 brain regions (cerebral cortex, corpus striatum, hypothalamus/thalamus and brainstem) and in heart ventricles were measured in rats chronically treated with nicotine added to the drinking water in doses ranging from 6 to 8 mg/kg/day, for 4 weeks. Control rats received only tap water. The nicotine treatment led to increases in the specific binding of both [3H]prazosin and [3H]clonidine in the cerebral cortex. An increase in [3H]prazosin binding was also observed in the hypothalamus/thalamus of nicotine-treated rats. These changes were all due to an increase of about 23% in Bmax. In the brainstem and heart left ventricle, respectively, an increase and a decrease in the affinity of [3H]quinuclidinyl benzilate binding were observed. There were no changes of the binding parameters for the 3 radioligands in other regions tested, and no alteration of [3H]dihydroalprenolol binding was detected in any region examined. These results indicate that chronic administration of nicotine causes an increase in the density of alpha 1- and alpha 2-binding sites in some brain regions and reciprocal changes of the affinity of muscarinic binding sites in the brain and in the heart.