酚妥拉明——兔子体内一种意想不到的激动剂。
Phentolamine--an unexpected agonist in the rabbit.
作者信息
Angus J A, Lew M J
出版信息
Br J Pharmacol. 1984 Mar;81(3):423-5. doi: 10.1111/j.1476-5381.1984.tb10094.x.
Abstract
Phentolamine (0.1-10 microM) caused an anomalous rightward shift of the relationship between the number of electrical field pulses and tachycardia in the rabbit isolated right atrium. Phentolamine was apparently acting as a presynaptic agonist on sympathetic nerve endings to inhibit transmitter release. The effect was prevented by benextramine treatment and antagonized 10 fold by yohimbine (1 microM) but not by prazosin (0.1 microM). In ganglion-blocked (mecamylamine) conscious or anaesthetized rabbits, phentolamine (3-1000 micrograms kg-1) caused a dose-related rise in blood pressure that was antagonized by yohimbine (1 mg kg-1). These pressor and inhibitory cardiac sympathetic nerve effects of phentolamine are not found in similar preparations from the guinea-pig or rat. Therefore, these rabbit-specific agonist effects of phentolamine at sites similar to alpha 2-adrenoceptors make this drug unsuitable as an alpha-adrenoceptor antagonist in rabbits.
摘要
酚妥拉明（0.1 - 10微摩尔）使家兔离体右心房中电场刺激次数与心动过速之间的关系出现异常右移。酚妥拉明显然是作为交感神经末梢的突触前激动剂来抑制递质释放。苯苄胺处理可阻止该效应，育亨宾（1微摩尔）可使其作用拮抗10倍，但哌唑嗪（0.1微摩尔）则无此作用。在神经节阻断（美加明）的清醒或麻醉家兔中，酚妥拉明（3 - 1000微克/千克）可引起剂量相关的血压升高，育亨宾（1毫克/千克）可拮抗此作用。酚妥拉明的这些升压和抑制心脏交感神经的作用在豚鼠或大鼠的类似标本中未发现。因此，酚妥拉明在类似于α2 - 肾上腺素能受体部位的这些家兔特异性激动剂作用，使得该药不适于作为家兔的α - 肾上腺素能受体拮抗剂。
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本文引用的文献
1
The determination of presynaptic pA2 values of yohimbine and phentolamine on the perfused rat heart under conditions of negligible autoinhibition.在自身抑制可忽略不计的条件下，测定育亨宾和酚妥拉明对灌注大鼠心脏的突触前pA2值。
Br J Pharmacol. 1983 May;79(1):109-19. doi: 10.1111/j.1476-5381.1983.tb10502.x.
2
Refractory period fluid stimulation of right atria: a method for studying presynaptic receptors in cardiac autonomic transmission.
J Pharmacol Methods. 1981 Aug;6(1):51-64. doi: 10.1016/0160-5402(81)90084-x.
3
Evidence against presynaptic alpha-adrenoreceptor modulation of cardiac sympathetic transmission.反对心脏交感神经传递中突触前α-肾上腺素能受体调节的证据。
Nature. 1980 Jul 17;286(5770):288-91. doi: 10.1038/286288a0.
4
Postsynaptic alpha 1- and alpha 2-adrenoceptors in the circulatory system of the pithed rat: selective stimulation of the alpha 2-type by B-HT 933.脊髓麻醉大鼠循环系统中的突触后α1和α2肾上腺素能受体：B-HT 933对α2型受体的选择性刺激
Eur J Pharmacol. 1980 May 2;63(2-3):199-202. doi: 10.1016/0014-2999(80)90446-x.
5
Species variation in vas deferens motor transmission [proceedings].
J Physiol. 1978 Aug;281:28P-29P.
6
Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.
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7
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Eur J Pharmacol. 1976 Apr;36(2):313-20. doi: 10.1016/0014-2999(76)90084-4.
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