AR-C 239对大鼠α1肾上腺素能受体阻断特性的进一步研究。

Further investigations on the alpha 1-adrenoceptor blocking properties of AR-C 239 in rats.

作者信息

Huchet A M, Andréjak M, Lucet B, Gautret B, Doursout M F, Ostermann G, Schmitt H

出版信息

Clin Exp Pharmacol Physiol. 1985 Sep-Oct;12(5):505-13. doi: 10.1111/j.1440-1681.1985.tb00901.x.

DOI:10.1111/j.1440-1681.1985.tb00901.x

Abstract

AR-C 239, a new alpha-adrenoceptor blocking drug, appears to act selectively on alpha 1 sites in rats. At peripheral sites, this drug did not change the tachycardia induced by spinal sympathetic outflow stimulation in pithed rats, and did not antagonize the inhibitory effects of clonidine on this preparation. In addition, AR-C 239 showed predominant alpha 1-adrenoceptor blocking properties in the bisected rat vas deferens preparation. AR-C 239 did not prevent or reverse the centrally mediated hypotensive and bradycardic actions induced by clonidine, in intact animals. In conclusion, AR-C 239 seems to be a very useful tool for the characterization of peripheral and central alpha 1-adrenoceptors, in this animal species.

摘要

AR-C 239是一种新型α-肾上腺素能受体阻断药物，在大鼠中似乎对α1位点具有选择性作用。在外周部位，该药物不会改变去脑大鼠脊髓交感神经传出刺激所诱发的心动过速，也不会拮抗可乐定对该标本的抑制作用。此外，在大鼠输精管二分标本中，AR-C 239表现出主要的α1-肾上腺素能受体阻断特性。在完整动物中，AR-C 239不能预防或逆转可乐定所诱发的中枢介导的降压和心动过缓作用。总之，对于在该动物物种中表征外周和中枢α1-肾上腺素能受体而言，AR-C 239似乎是一种非常有用的工具。

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