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α₂肾上腺素能受体选择性激动剂B-HT 920和UK 14,304在大鼠和豚鼠主动脉条中诱导的收缩是由α₁肾上腺素能受体介导的。

The contractions induced in rat and guinea-pig aortic strips by the alpha 2-adrenoceptor selective agonists B-HT 920 and UK 14,304 are mediated by alpha 1-adrenoceptors.

作者信息

Beckeringh J J, Thoolen M J, De Jonge A, Wilffert B, Timmermans P B, Van Zwieten P A

出版信息

Eur J Pharmacol. 1984 Sep 17;104(3-4):197-203. doi: 10.1016/0014-2999(84)90394-7.

DOI:10.1016/0014-2999(84)90394-7
PMID:6149946
Abstract

The alpha-adrenergic action of the selective alpha 2-adrenoceptor agonists B-HT 920 and UK 14,304 was investigated on helically cut preparations of rat and guinea-pig isolated aorta. The alpha 1-adrenoceptor selective stimulant (-)-phenylephrine was included for comparison. All agonists induced concentration-dependent contractions in both preparations. Calcium entry blockade by D 600 almost abolished the contractions evoked by B-HT 920 and UK 14,304 in rat aorta while those evoked in guinea-pig aorta were less strongly affected. Contractions elicited by (-)-phenylephrine were moderately impaired by D 600 in rat aorta whereas there was only a limited effect in guinea-pig aorta. Analysis of the prazosin and yohimbine antagonism of B-HT 920- and UK 14,304-evoked contractions showed the involvement of alpha 1-like adrenoceptors in rat and guinea-pig aorta, prazosin being approximately 1000 times more potent that yohimbine. The results show that B-HT 920 and UK 14,304 contract rat and guinea-pig aorta via alpha 1-like adrenoceptors which are not identical. It is submitted that rat and guinea-pig alpha 1-adrenoceptors activate different contractile processes.

摘要

在大鼠和豚鼠离体主动脉的螺旋切片标本上研究了选择性α₂ - 肾上腺素能受体激动剂B - HT 920和UK 14,304的α - 肾上腺素能作用。将α₁ - 肾上腺素能受体选择性激动剂（-）-去氧肾上腺素纳入进行比较。所有激动剂在两种标本中均诱导出浓度依赖性收缩。D 600对钙内流的阻断几乎消除了B - HT 920和UK 14,304在大鼠主动脉中引起的收缩，而在豚鼠主动脉中引起的收缩受影响较小。D 600使（-）-去氧肾上腺素在大鼠主动脉中引起的收缩适度减弱，而在豚鼠主动脉中只有有限的作用。对B - HT 920和UK 14,304引起的收缩的哌唑嗪和育亨宾拮抗作用分析表明，大鼠和豚鼠主动脉中存在α₁样肾上腺素能受体，哌唑嗪的效力比育亨宾强约1000倍。结果表明，B - HT 920和UK 14,304通过不同的α₁样肾上腺素能受体使大鼠和豚鼠主动脉收缩。认为大鼠和豚鼠的α₁ - 肾上腺素能受体激活不同的收缩过程。

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1
The contractions induced in rat and guinea-pig aortic strips by the alpha 2-adrenoceptor selective agonists B-HT 920 and UK 14,304 are mediated by alpha 1-adrenoceptors.α₂肾上腺素能受体选择性激动剂B-HT 920和UK 14,304在大鼠和豚鼠主动脉条中诱导的收缩是由α₁肾上腺素能受体介导的。
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