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在α-肾上腺素能受体拮抗作用测量中使用神经释放的激动剂。

The use of neurally released agonist in the measurement of antagonism at alpha-adrenoceptors.

作者信息

French A M, Scott N C

出版信息

Br J Pharmacol. 1983 Dec;80(4):655-61. doi: 10.1111/j.1476-5381.1983.tb10055.x.

DOI:10.1111/j.1476-5381.1983.tb10055.x
PMID:6152828
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2045051/
Abstract

Graded contractile responses of the rat vas deferens were obtained to trains containing varying numbers of pulses delivered transmurally at 500 Hz, allowing construction of pulse-response curves. In the presence of postjunctional adrenoceptor blocking drugs, these curves were displaced to the right in a parallel manner, allowing the estimation of pA2 values for the drugs. Activity of drugs at prejunctional adrenoceptors was estimated from the reduction of inhibition of the response to a second pulse delivered 3 s after trains containing different numbers of pulses. It is suggested that the technique is more physiological than others used to determine the antagonistic activity of drugs at adrenoceptors.

摘要

在500Hz频率下经壁施加含有不同脉冲数的串刺激,可获得大鼠输精管的分级收缩反应,从而构建脉冲-反应曲线。在存在节后肾上腺素能受体阻断药物的情况下,这些曲线以平行方式向右移位,由此可估算药物的pA2值。通过含有不同脉冲数的串刺激后3秒施加的第二个脉冲反应抑制的降低,来估算药物在节前肾上腺素能受体的活性。有人认为,该技术比用于测定药物对肾上腺素能受体拮抗活性的其他技术更具生理性。

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本文引用的文献

1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
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Conditions required for the inhibitory feedback loop in noradrenergic transmission.去甲肾上腺素能传递中抑制性反馈回路所需的条件。
Nature. 1981 Sep 3;293(5827):62-5. doi: 10.1038/293062a0.
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Prazosin selectively inhibits the responses to field stimulation in the rat vas deferens.哌唑嗪可选择性抑制大鼠输精管对场刺激的反应。
Eur J Pharmacol. 1981 May 22;71(4):447-53. doi: 10.1016/0014-2999(81)90189-8.
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alpha 1-adrenoceptors can mediate chronotropic responses in the rat heart.α1肾上腺素能受体可介导大鼠心脏的变时反应。
Br J Pharmacol. 1981 Jul;73(3):586-8. doi: 10.1111/j.1476-5381.1981.tb16791.x.
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Feedback inhibition of responses of rat vas deferens to twin pulse stimulation.大鼠输精管对双脉冲刺激反应的反馈抑制
Eur J Pharmacol. 1983 Jan 21;86(3-4):379-83. doi: 10.1016/0014-2999(83)90187-5.
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Evidence to support the hypothesis that ATP is a co-transmitter in rat vas deferens.支持ATP是大鼠输精管共递质这一假说的证据。
Experientia. 1983 Mar 15;39(3):264-6. doi: 10.1007/BF01955295.
8
The influence of neuronal uptake upon the relative potencies of agonists acting at prejunctional alpha 2-adrenoceptors in the rat isolated vas deferens.神经元摄取对作用于大鼠离体输精管突触前α2肾上腺素能受体的激动剂相对效价的影响。
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A comparison of pre- and post-junctional potencies of several alpha-adrenoceptor agonists in the cardiovascular system and anococcygeus muscle of the rat. Evidence for two types of post-junctional alpha-adrenoceptor.几种α-肾上腺素能激动剂在大鼠心血管系统和尾骨肌中节前和节后效能的比较。两种节后α-肾上腺素能受体的证据。
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10
Methoxamine as a tool to assess the importance of intraneuronal uptake of l-norepinephrine in the cat's nictitating membrane.甲氧明作为一种工具,用于评估猫瞬膜中去甲肾上腺素的神经元内摄取的重要性。
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