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神经元摄取抑制剂对胍乙啶在兔输精管中产生的肾上腺素能神经元阻滞作用的影响。

Effect of neuronal uptake inhibitors on the adrenergic-neuron blockade produced by guanethidine in rabbit vas deferens.

作者信息

Huston L J, Golko D S, Paton D M

出版信息

Can J Physiol Pharmacol. 1977 Jun;55(3):609-14. doi: 10.1139/y77-084.

DOI:10.1139/y77-084
PMID:884617
Abstract

The effect of neuronal-uptake inhibitors on the guanethidine-induced inhibition of responses of rabbit vas deferens to transmural stimulation was investigated. The twitch and sustained responses were inhibited by about 70% by 1.2 X 10(-5) M guanethidine. Prior or subsequent exposure to the noradrenaline-uptake inhibitors, 3.3 X 10(-5) M cocaine, 10(-5)M nisoxetine, and 10(-7)M desipramine prevented or reversed these effects of guanethidine. The depressant effects of guanethidine were not modified by the serotonin-uptake inhibitor, 10(-6)M fluoxetine. The uptake of 5 X 10(-8)M (-)-[3H]noradrenaline by rabbit vas deferens was significantly reduced by guanethidine, cocaine, nisoxetine, and desipramine, but not by fluoxetine. It was concluded that guanethidine inhibited both the twitch and sustained responses of the vas by producing adrenergic-neuron blockade and that these effects were dependent on continued transport into adrenergic neurons.

摘要

研究了神经元摄取抑制剂对胍乙啶诱导的兔输精管对跨壁刺激反应抑制的影响。1.2×10⁻⁵ M胍乙啶可使抽搐反应和持续反应受到约70%的抑制。预先或随后暴露于去甲肾上腺素摄取抑制剂、3.3×10⁻⁵ M可卡因、10⁻⁵ M尼索西汀和10⁻⁷ M地昔帕明可预防或逆转胍乙啶的这些作用。5-羟色胺摄取抑制剂10⁻⁶ M氟西汀并未改变胍乙啶的抑制作用。胍乙啶、可卡因、尼索西汀和地昔帕明可显著降低兔输精管对5×10⁻⁸ M(-)-[³H]去甲肾上腺素的摄取,但氟西汀无此作用。得出的结论是,胍乙啶通过产生肾上腺素能神经元阻滞来抑制输精管的抽搐反应和持续反应,且这些作用依赖于其持续转运至肾上腺素能神经元。

相似文献

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Effect of neuronal uptake inhibitors on the adrenergic-neuron blockade produced by guanethidine in rabbit vas deferens.神经元摄取抑制剂对胍乙啶在兔输精管中产生的肾上腺素能神经元阻滞作用的影响。
Can J Physiol Pharmacol. 1977 Jun;55(3):609-14. doi: 10.1139/y77-084.
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Further studies on the adrenergic neuron blocking activity of some -adrenoceptor antagonists and guanethidine.某些β-肾上腺素能受体拮抗剂和胍乙啶对肾上腺素能神经元阻断活性的进一步研究。
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The potentiating effects of 4-aminopyridine on adrenergic transmission in the rabbit vas deferens.4-氨基吡啶对家兔输精管肾上腺素能传递的增强作用。
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Activation and desensitization of presynaptic alpha 2-adrenoceptors after inhibition of neuronal uptake by antidepressant drugs in the rat vas deferens.抗抑郁药抑制大鼠输精管神经元摄取后突触前α₂-肾上腺素能受体的激活与脱敏
Br J Pharmacol. 1986 Dec;89(4):673-83. doi: 10.1111/j.1476-5381.1986.tb11171.x.

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J Cell Biol. 1978 Oct;79(1):121-31. doi: 10.1083/jcb.79.1.121.