溴苄铵通过钠敏感主动转运进入肾上腺素能神经元，用于兔回肠中阻滞作用的产生。

Sodium sensitive active transport of bretylium into adrenergic neurons for the development of blockade in rabbit ileum.

作者信息

Hosotani T, Misu Y

出版信息

Arch Int Pharmacodyn Ther. 1977 Apr;226(2):235-45.

Abstract

Transport of bretylium into adrenergic neurons was studied, using rabbit isolated periarterial nerve ileum preparations, by determining the effects of various incubation procedures, which inhibit noradrenaline uptake, to prevent or reverse the blockade. Adrenergic neuron blockade by bretylium 5 X 10(-5) (g/ml) was prevented but not reversed by incubation with sodium free and low temperature (10 degrees C) media. Ouabain 2.2 X 10(-8) and anoxia prevented bretylium-induced blockade. Noradrenaline 5 X 10(-6) and 8 X 10(-5) prevented and also reversed the blockade, but the reversing effect was transient. High calcium (totally 10 mM) readily reversed the bretylium-induced blockade, the recovery being complete and long-lasting. In light of the results, a sodium sensitive active transport of bretylium into adrenergic neurons is apparently necessary for development of adrenergic neuron blocking action in rabbit ilea.

摘要

利用兔离体动脉周围神经回肠制备物，通过测定各种抑制去甲肾上腺素摄取的孵育程序对预防或逆转阻断作用的影响，研究了溴苄铵向肾上腺素能神经元的转运。用无钠和低温（10℃）培养基孵育可预防但不能逆转5×10⁻⁵（g/ml）溴苄铵引起的肾上腺素能神经元阻断。哇巴因2.2×10⁻⁸和缺氧可预防溴苄铵诱导的阻断。5×10⁻⁶和8×10⁻⁵的去甲肾上腺素可预防并逆转阻断，但逆转作用是短暂的。高钙（总量10 mM）可轻易逆转溴苄铵诱导的阻断，恢复完全且持久。根据这些结果，在兔回肠中，溴苄铵向肾上腺素能神经元的钠敏感主动转运显然是其产生肾上腺素能神经元阻断作用所必需的。