鹅膏蕈氨酸拮抗鬼笔环肽诱导的负性肌力作用，并在电压钳制的青蛙肌肉纤维中电压依赖性地阻断快速外向钾电流。

Antamanide antagonizes the phalloidin-induced negative inotropic effect and blocks voltage dependently the fast outward K+ current in voltage-clamped frog muscle fibres.

作者信息

Raymond G, Potreau D, Cognard C, Jahn W, Wieland T

出版信息

Eur J Pharmacol. 1987 Jun 12;138(1):21-7. doi: 10.1016/0014-2999(87)90332-3.

PMID:2442001

Abstract

The effects of antamanide (10(-14)-10(-5) M) and N-acetyl-secophalloidin (10(-7)-5 X 10(-3) M) a neutral non-toxic derivative of phalloidin, were tested on voltage-clamped single frog muscle fibres. Antamanide protected muscle fibres against the negative inotropic effect of phalloidin but blocked the fast potassium permeability in the same concentration range and the same voltage-dependent manner as did phalloidin. N-Acetyl-secophalloidin exhibited a strongly attenuated blocking effect on K+ permeability in a 1,000-fold higher concentration range than phalloidin. Neither antamanide nor N-acetyl-secophalloidin affected the contractile properties. These results suggest the existence in the frog muscle membrane of a receptor with two sites for phalloidin and antamanide which acts on potassium conductance.

摘要

在电压钳制的单根蛙肌纤维上测试了鹅膏毒环肽（10⁻¹⁴ - 10⁻⁵ M）和鬼笔环肽的中性无毒衍生物N - 乙酰 - 去甲鬼笔环肽（10⁻⁷ - 5×10⁻³ M）的作用。鹅膏毒环肽可保护肌纤维免受鬼笔环肽的负性肌力作用，但在相同浓度范围内且以与鬼笔环肽相同的电压依赖性方式阻断快速钾通透性。N - 乙酰 - 去甲鬼笔环肽在比鬼笔环肽高1000倍的浓度范围内对钾通透性表现出强烈减弱的阻断作用。鹅膏毒环肽和N - 乙酰 - 去甲鬼笔环肽均不影响收缩特性。这些结果表明，在蛙肌膜中存在一种对鬼笔环肽和鹅膏毒环肽有两个作用位点的受体，该受体作用于钾电导。