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4-氨基吡啶对离体输精管的作用及其对腺苷、吗啡、去甲肾上腺素和γ-氨基丁酸抑制特性的影响。

The effects of 4-aminopyridine on the isolated vas deferens and its effects on the inhibitory properties of adenosine, morphine, noradrenaline and gamma-aminobutyric acid.

作者信息

Stone T W

出版信息

Br J Pharmacol. 1981 Jul;73(3):791-6. doi: 10.1111/j.1476-5381.1981.tb16817.x.

Abstract

1 Adenosine, adenosine 5'-triphosphate (ATP), morphine, noradrenaline, gamma-aminobutyric acid (GABA) phentolamine and amyl nitrite were used to inhibit electrically-evoked contractions of the isolated superfused vas deferens of the mouse. 2 The inhibitory effects of adenosine ATP, morphine, noradrenaline and GABA, which are thought to be due to presynaptic action, were reduced by perfusion with media containing 4-aminopyridine (4AP) or tetraethylammonium (TEA) ions. The inhibitory effects of phentolamine and amyl nitrite were unaffected by 4AP or TEA. 3 Quinidine, which like 4AP and TEA produced some increase to twitch height, did not reduce responses to the various agonists, indicating that an increased muscle contraction was not itself responsible for the reduced responses. 4 It is concluded that antagonism between 4AP and adenosine is not a specific interaction, as had been suggested, but probably reflects an interaction with Ca2+ requiring processes in the presynaptic terminal.

摘要
  1. 腺苷、腺苷5'-三磷酸(ATP)、吗啡、去甲肾上腺素、γ-氨基丁酸(GABA)、酚妥拉明和亚硝酸异戊酯被用于抑制小鼠离体灌流输精管的电诱发收缩。2. 腺苷、ATP、吗啡、去甲肾上腺素和GABA的抑制作用被认为是由于突触前作用,用含有4-氨基吡啶(4AP)或四乙铵(TEA)离子的培养基灌注可降低其抑制作用。酚妥拉明和亚硝酸异戊酯的抑制作用不受4AP或TEA的影响。3. 奎尼丁与4AP和TEA一样,使抽搐高度有所增加,但并未降低对各种激动剂的反应,这表明肌肉收缩增强本身并不是反应降低的原因。4. 得出的结论是,4AP与腺苷之间的拮抗作用并非如所认为的那样是一种特异性相互作用,而可能反映了与突触前终末中需要Ca2+的过程的相互作用。

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