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胍乙啶与右旋苯丙胺之间的拮抗作用机制。

Mechanism of the antagonism between guanethidine and dexamphetamine.

作者信息

Gerkens J F, McCulloch M W

出版信息

Br J Pharmacol. 1969 Mar;35(3):563-72. doi: 10.1111/j.1476-5381.1969.tb08297.x.

Abstract
  1. The effects of dexamphetamine were studied on the responses of rabbit ileum, rabbit ear artery and sheep spleen to sympathetic nerve stimulation after exposure to guanethidine and in the absence of guanethidine.2. In the absence of guanethidine, dexamphetamine enhanced the responses to sympathetic stimulation and, in the spleen, this was shown to be due to an increase in noradrenaline output. However, the increase in these responses was much less than the increase obtained in preparations treated with guanethidine.3. Cocaine, in a concentration which produced the same effect on noradrenaline uptake as the concentration of dexamphetamine used, was also effective in reversing the adrenergic neurone blocking actions of guanethidine.4. It is suggested that the antagonism between dexamphetamine and guanethidine is due to a reduction in the uptake of guanethidine by the nerve endings rather than to interaction of the two drugs at the receptor site for the adrenergic neurone blocking action of guanethidine.
摘要
  1. 研究了右旋苯丙胺对暴露于胍乙啶后以及未暴露于胍乙啶时兔回肠、兔耳动脉和羊脾脏对交感神经刺激的反应的影响。

  2. 在未使用胍乙啶的情况下,右旋苯丙胺增强了对交感神经刺激的反应,在脾脏中,这被证明是由于去甲肾上腺素输出增加所致。然而,这些反应的增加远小于用胍乙啶处理的制剂中获得的增加。

  3. 可卡因在产生与所用右旋苯丙胺浓度相同的去甲肾上腺素摄取作用的浓度下,也能有效逆转胍乙啶的肾上腺素能神经元阻断作用。

  4. 有人提出,右旋苯丙胺与胍乙啶之间的拮抗作用是由于神经末梢对胍乙啶的摄取减少,而不是由于这两种药物在胍乙啶肾上腺素能神经元阻断作用的受体部位相互作用。

相似文献

3
Evidence for a competitive antagonism of guanethidine by dexamphetamine.右旋苯丙胺对胍乙啶竞争性拮抗作用的证据。
Br J Pharmacol Chemother. 1963 Feb;20(1):17-28. doi: 10.1111/j.1476-5381.1963.tb01293.x.

引用本文的文献

1
Guanethidine after twenty years: a pharmacologist's perspective.二十年后的胍乙啶:一位药理学家的视角
Br J Clin Pharmacol. 1982 Jan;13(1):35-44. doi: 10.1111/j.1365-2125.1982.tb01334.x.

本文引用的文献

1
On the nature of inhibition in the intestine.论肠道抑制的本质。
J Physiol. 1930 Sep 18;70(2):145-57. doi: 10.1113/jphysiol.1930.sp002683.
4
Evidence for a competitive antagonism of guanethidine by dexamphetamine.右旋苯丙胺对胍乙啶竞争性拮抗作用的证据。
Br J Pharmacol Chemother. 1963 Feb;20(1):17-28. doi: 10.1111/j.1476-5381.1963.tb01293.x.

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