Inhibitory effects of tetrahydroisoquinoline derivatives on Ca2+ and Na+ channels in crude nerve endings

被引：0
|
作者：
Zhang, Y
Abe, J
Wada, T
Ichida, S
Xu, GY
机构：
[1] Kinki Univ, Fac Pharmaceut Sci, Dept Biol Chem, Higashiosaka, Osaka 5778502, Japan
[2] China Pharmaceut Univ, Coll Pharm, Div Med Chem, Nanjing 210009, Peoples R China
来源：
BIOLOGICAL & PHARMACEUTICAL BULLETIN | 2000年 / 23卷 / 03期
关键词：
isoquinoline; calcium ion channel; sodium ion channel; calmodulin-dependent phosphodiesterase (CaM-PDE);
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Semi-synthetic tetrahydroisoquinoline derivatives prepared from natural alkaloids, possess Ca2+ antagonistic properties. These derivatives significantly blocked KCl-stimulated Ca2+ uptake (In chick and rat crude nerve endings) which fan be partially inhibited by the selective N-type Ca2+ channel blocker omega-conotoxin GVIA or the selective P-type Ca2+ channel blocker omega-agatoxin IVA. Moreover, PX42 (10 mu M; for the tetrahydroisoquinoline compounds in this study) could inhibit the activity of calmodulin-dependent phosphodiesterase and block veratridine-induced (or tetrodotoxin-sensitive) Na+ uptake. The possible mechanism(s) of non-selective inhibition of ion channels of PX42 is discussed.
引用
收藏
页码：375 / 378
页数：4
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