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人唇唾液腺中毒蕈碱型乙酰胆碱受体的特征分析

Characterization of muscarinic acetylcholine receptors in human labial salivary glands.

作者信息

Mei L, Roeske W R, Izutsu K T, Yamamura H I

机构信息

Department of Pharmacology, University of Arizona Health Sciences Center, Tucson 85724.

出版信息

Eur J Pharmacol. 1990 Feb 13;176(3):367-70. doi: 10.1016/0014-2999(90)90032-2.

DOI:10.1016/0014-2999(90)90032-2
PMID:2328757
Abstract

Muscarinic acetylcholine receptors were studied in human labial salivary glands with (-)-[3H]MQNB. The radioligand bound with a Kd value of 150 pM. The density of muscarinic receptors was 220 fmol/mg protein. Most muscarinic antagonists bound to a homogeneous population of muscarinic receptors in this tissue. However, the inhibition curves of pirenzepine had a Hill slope of 0.57 and could be analyzed by a two site model. These results suggest that the muscarinic receptors in human labial salivary glands are a mixture of M1 and M3 types.

摘要

用(-)-[³H]甲基喹啉酮对人唇唾液腺中的毒蕈碱型乙酰胆碱受体进行了研究。放射性配体结合的解离常数(Kd)值为150皮摩尔。毒蕈碱受体的密度为220飞摩尔/毫克蛋白质。在该组织中,大多数毒蕈碱拮抗剂与毒蕈碱受体的同质群体结合。然而,哌仑西平的抑制曲线的希尔斜率为0.57,并且可以用双位点模型进行分析。这些结果表明,人唇唾液腺中的毒蕈碱受体是M1型和M3型的混合物。

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