Decrease or increase in cardiac muscarinic cholinergic receptor number in rats treated with methacholine or atropine

作者: Bradley C. Wise , Mamoru Shoji , J.F. Kuo

DOI: 10.1016/0006-291X(80)90405-2

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摘要: The effects of chronic treatment the rat with methacholine and atropine on cardiac muscarinic cholinergic receptors were investigated. [3H]Quinuclidinyl benzilate ([3H]QNB) was used to directly estimate number affinity in heart ventricular membrane. Methacholine decreased, a dose-related time-dependent manner, specific binding [3H]QNB by 34% as compared control. Atropine treatment, other hand, resulted increase (28 66%) receptors. equilibrium dissociation constant (KD) for ligand same (about 200 pM) control treated groups rats, whereas (39 105%) KD noted rats. Similarly, concentration acetylcholine causing 50 percent inhibition (IC50) unaltered rats (4 μM), but it increased 43%

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