摘要
以最小反应模型分析ＨＩ６抗骨骼肌烟碱受体的作用陈厚昌，白敦衍１，蒋毅萍（第一军医大学药理教研室，１计算机教研室，广州５１０５１５，中国）关键词ＨＩ６；骨骼肌；胆碱能受体；信使ＲＮＡ；非洲爪蟾；卵母细胞目的：研究１（２ｈｙｄｒｏｘｙｉｍｉｎｏｍ...
IM: To study the action of 1 (2 hydroxyimino￣methyl 1
pyridino) 3 (4 carbamoyl 1 pyridino) 2 oxapropane dichloride
(HI 6) on skeletal muscle acetylcholine receptor (N 2 ChR).
METHODS: N 2 ChR was expressed in Xenopus laevis oocyte after
injection with mRNA extracted from denervated rat leg muscles. The
inward membrane currents induced by various concentrations of
carbamylcholine and effects of HI 6 or d tubocurarine on the
currents were measured with voltage clamp technique by fast cell flow
of agents. The actions of HI 6 and d tubocurarine on N 2 ChR
were analyzed by using the minimal reaction model. RESULTS: K of
40 05, 156 00, and 334 67 μmol·L -1 for HI 6, K of 0
02, 0 10, and 0 18 μmol·L -1 for d tubocurarine were
obtained by using the competing for single acetylcholine (ACh)
binding site model, the competing for two ACh binding sites model,
and the noncompetitive inhibition model, respectively. CONCLUSION: HI
6 and d tubocurarine competed for two ACh binding sites of N 2
ChR with equal affinity to antagonize the effects of the agonist on N
2 ChR. The N 2 ChR inhibition by HI 6 is much weaker than that by
d tubocurarine.
出处
《中国药理学报》
CSCD
1996年第5期428-431,共4页
Acta Pharmacologica Sinica
关键词
HI-6
骨骼肌
胆碱能
受体
信使
RNA
卵母细胞
HI 6
skeletal muscle
cholinergic receptors
messenger
RNA
Xenopus laevis
oocytes
