毒蕈碱型乙酰胆碱受体介导的腺苷酸环化酶活性调节
Regulation of adenylate cyclase activity mediated by muscarinic acetylcholine receptors.
作者信息
Nathanson N M, Klein W L, Nirenberg M
出版信息
Proc Natl Acad Sci U S A. 1978 Apr;75(4):1788-91. doi: 10.1073/pnas.75.4.1788.
Abstract
Carbachol, an activator of muscarinic acetylcholine receptors of NG108-15 hybrid cells, inhibits adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] rapidly and reversibly and slowly evokes a 200-300% increase in adenylate cyclase activity over a period of 24-30 hr. Both the inhibition of adenylate cyclase and the gradual increase in enzyme activity are dependent on muscarinic acetylcholine receptors and the receptor activator. Withdrawal of carbachol results in a gradual return of adenylate cyclase activity to control levels over a period of 6 hr; the half-life for decay of enzyme activity is 1.6 hr. These results show that muscarinic acetylcholine receptors mediate both transient and long-lived effects on adenylate cyclase activity that resemble those of opiates.
摘要
卡巴胆碱是NG108 - 15杂交细胞毒蕈碱型乙酰胆碱受体的激活剂，它能快速、可逆地抑制腺苷酸环化酶[ATP焦磷酸裂解酶（环化），EC 4.6.1.1]，并在24 - 30小时内缓慢引起腺苷酸环化酶活性增加200 - 300%。腺苷酸环化酶的抑制作用和酶活性的逐渐增加均依赖于毒蕈碱型乙酰胆碱受体和受体激活剂。撤去卡巴胆碱后，腺苷酸环化酶活性在6小时内逐渐恢复到对照水平；酶活性衰减的半衰期为1.6小时。这些结果表明，毒蕈碱型乙酰胆碱受体介导了对腺苷酸环化酶活性的短暂和长期影响，这些影响类似于阿片类药物的作用。
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