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地昔帕明对α-肾上腺素能受体拮抗剂对三段大鼠输精管收缩反应影响的修饰作用。

Modification by desipramine of the effects of alpha-adrenoceptor antagonists on the contractile responses of the trisected rat vas deferens.

作者信息

Bradley L, Doggrell S A

出版信息

Gen Pharmacol. 1985;16(5):475-82. doi: 10.1016/0306-3623(85)90007-2.

Abstract

Desipramine at 10(-7) M inhibited the neuronal uptake of noradrenaline and at 10(-6) M was also a alpha 1-adrenoceptor blocker. Desipramine potentiated and inhibited the responses of the epididymal and other portions to field stimulation, respectively, probably because the increased concentration of noradrenaline in the synapse was stimulating postjunctional alpha 1- and prejunctional alpha 2-adrenoceptors, respectively. Qualitatively the effects of prazosin, phentolamine and yohimbine on responses to added noradrenaline and to field stimulation were consistent with their being alpha 1-selective, nonselective and alpha 2-selective adrenoceptor antagonists. Quantitatively the effects of phentolamine and/or yohimbine on fast and slow responses to field stimulation and the modification of these effects by desipramine were dependent on the portion of vas, the response, the frequency of stimulation and the concentration of desipramine used.

摘要

10⁻⁷M的地昔帕明抑制去甲肾上腺素的神经元摄取,而10⁻⁶M的地昔帕明还是一种α₁ - 肾上腺素能受体阻滞剂。地昔帕明分别增强和抑制附睾及其他部位对场刺激的反应,这可能是因为突触中去甲肾上腺素浓度升高分别刺激了突触后α₁ - 肾上腺素能受体和突触前α₂ - 肾上腺素能受体。定性地说,哌唑嗪、酚妥拉明和育亨宾对添加去甲肾上腺素和场刺激反应的影响与其作为α₁选择性、非选择性和α₂选择性肾上腺素能受体拮抗剂的特性一致。定量地说,酚妥拉明和/或育亨宾对场刺激快速和慢速反应的影响以及地昔帕明对这些影响的改变取决于血管的部位、反应、刺激频率以及所用的地昔帕明浓度。

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