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  • Title: Modulation by nicotine on binding of cerebral muscarinic receptors with muscarinic agonist and antagonist.
    Author: Wang H, Cui WY, Liu CH.
    Journal: Zhongguo Yao Li Xue Bao; 1996 Nov; 17(6):497-9. PubMed ID: 9863140.
    Abstract:
    AIM: To study the modulatory effects of nicotine on the binding of brain muscarinic receptors. METHODS: The binding of brain muscarinic receptors with the agonist [3H] oxotremorine-M or the antagonist l-[3H]QNB was determined in the presence/absence of nicotine. RESULTS: Pre-incubation of the membrane fraction derived from rat cerebral cortex with nicotine 1.0 mumol.L-1 led to a decrease in the dissociation constant (Kd) for [3H] oxotremorine-M binding to muscarinic receptors, while the maximal binding value (Bmax) was unchanged. The Kd value for binding of the muscarinic antagonist l-[3H]QNB was concentration-dependently increased by preincubation with nicotine 0.1 nmol.L-1-10.0 mumol.L-1, with Bmax unchanged. The effect of nicotine on the Kd for l-[3H]QNB binding was prevented by mecamylamine 10 nmol.L-1, but was enhanced by dithiothreitol 10 mumol.L-1, which by itself was also capable of increasing the Kd value. CONCLUSION: Nicotine increases the affinity of brain muscarinic receptors for muscarinic agonist, but decreases the affinity of brain muscarinic receptors for muscarinic antagonist.
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