胆碱是一种通过毒蕈碱M1受体诱导神经元型一氧化氮合酶激活的完全激动剂。

Choline is a full agonist in inducing activation of neuronal nitric oxide synthase via the muscarinic M1 receptor.

作者信息

Carriere J L, El-Fakahany E E

机构信息

Division of Neuroscience Research in Psychiatry, Medical School, University of Minnesota, Minneapolis, MN 55455, USA.

出版信息

Pharmacology. 2000 Feb;60(2):82-9. doi: 10.1159/000028351.

DOI:10.1159/000028351

PMID:10657757

Abstract

The present study was designed to characterize the interaction of choline with the M(1) subtype of the muscarinic acetylcholine receptor. Using Chinese hamster ovary cells transfected with neuronal nitric oxide synthase and the cloned human M(1) receptor (CHO hM(1)/nNOS cells), we investigated choline's effects on production of nitric oxide and elevation of intracellular [Ca(2+)]. Choline showed the properties of a full agonist in inducing the sustained plateau of increased intracellular [Ca(2+)], although it was only a partial agonist in inducing the larger, transient [Ca(2+)] peak. Choline was also found to act as a full agonist in stimulating the production of nitric oxide. These results have implications for efforts in the clinical treatment of dementia.

摘要

本研究旨在表征胆碱与毒蕈碱型乙酰胆碱受体M(1)亚型之间的相互作用。利用转染了神经元型一氧化氮合酶和克隆的人M(1)受体的中国仓鼠卵巢细胞（CHO hM(1)/nNOS细胞），我们研究了胆碱对一氧化氮产生和细胞内[Ca(2+)]升高的影响。胆碱在诱导细胞内[Ca(2+)]持续升高的平台期时表现出完全激动剂的特性，尽管它在诱导较大的瞬时[Ca(2+)]峰值时只是部分激动剂。胆碱在刺激一氧化氮产生方面也被发现可作为完全激动剂。这些结果对痴呆症的临床治疗研究具有启示意义。