乙酰砷胆碱：一种胆碱能激动剂。

Acetylarsenocholine: a cholinergic agonist.

作者信息

Hedlund B, Norin H, Christakopoulos A, Alberts P, Bartfai T

出版信息

J Neurochem. 1982 Sep;39(3):871-3. doi: 10.1111/j.1471-4159.1982.tb07973.x.

DOI:10.1111/j.1471-4159.1982.tb07973.x

Abstract

The pharmacological properties of acetylarsenocholine, an arsenic analogue of acetylcholine, were investigated. Acetylarsenocholine behaved as a cholinergic ligand both in the central and peripheral nervous system. It bound to nicotinic receptors in rat medulla-pons with a KD of 15 microM and to muscarinic receptors in rat cerebral cortex with a KD of 10 microM. It behaved also as an agonist at presynaptic muscarinic receptors in guinea pig ileum myenteric plexus preparation. Arsenocholine is an alternative substrate for choline acetyltransferase and acetylarsenocholine is an alternative substrate for acetylcholinesterase.

摘要

对乙酰胆碱的砷类似物乙酰砷胆碱的药理特性进行了研究。乙酰砷胆碱在中枢和外周神经系统中均表现为胆碱能配体。它以15微摩尔的解离常数（KD）与大鼠延髓-脑桥中的烟碱受体结合，并以10微摩尔的KD与大鼠大脑皮层中的毒蕈碱受体结合。在豚鼠回肠肌间神经丛制备中，它在突触前毒蕈碱受体处也表现为激动剂。砷胆碱是胆碱乙酰转移酶的替代底物，而乙酰砷胆碱是乙酰胆碱酯酶的替代底物。