Purdy R E, Stupecky G L
J Pharmacol Exp Ther. 1984 May;229(2):459-68.
The alpha adrenoceptor properties of the rabbit ear artery and thoracic aorta were assessed using isolated blood vessel rings mounted in tissue baths. ED50 values and dissociation constants for norepinephrine (NE), epinephrine (EPI), isoproterenol (ISO), methoxamine (MET) and clonidine (CLO) were determined by analysis of dose-response data with and without partial inactivation of alpha receptors by phenoxybenzamine. The order of affinity of these agonists for the alpha receptors of ear artery was CLO less than EPI = NE = MET much less than ISO, and that in aorta was EPI less than NE less than CLO less than MET less than ISO. Alpha receptor reserves were larger in ear artery than aorta by factors of 182, 17, 7, 3.8 and 2 for EPI, NE, ISO, MET and CLO, respectively. In contrast, the fraction of receptors occupied at threshold contractile response was larger in aorta than ear artery with every agonist studied except CLO. The maximal response to the partial agonist, CLO, expressed as a fraction of the maximal response to NE in each vessel, was nearly 1.8 times greater in ear artery than in aorta. It is concluded that the alpha receptors of rabbit ear artery are qualitatively different from those of the thoracic aorta. In addition, the larger receptor reserves, smaller fraction of receptors occupied at threshold and the larger maximal response of CLO in ear artery support the hypothesis that alpha receptor density in this vessel is greater than that in the aorta.
利用安装在组织浴槽中的离体血管环评估兔耳动脉和胸主动脉的α肾上腺素能受体特性。通过分析在有无苯氧苄胺使α受体部分失活情况下的剂量反应数据,测定去甲肾上腺素(NE)、肾上腺素(EPI)、异丙肾上腺素(ISO)、甲氧明(MET)和可乐定(CLO)的半数有效剂量(ED50)值和解离常数。这些激动剂对耳动脉α受体的亲和力顺序为CLO<EPI = NE = MET<<ISO,而在主动脉中的顺序为EPI<NE<CLO<MET<ISO。对于EPI、NE、ISO、MET和CLO,耳动脉中的α受体储备分别比主动脉大182、17、7、3.8和2倍。相反,除CLO外,在所研究的每种激动剂作用下,主动脉在阈收缩反应时被占据的受体分数比耳动脉大。部分激动剂CLO的最大反应,以其在每条血管中相对于NE最大反应的分数表示,在耳动脉中比在主动脉中几乎大1.8倍。结论是兔耳动脉的α受体在性质上与胸主动脉的α受体不同。此外,耳动脉中较大的受体储备、阈反应时较小的被占据受体分数以及CLO较大的最大反应支持了该血管中α受体密度大于主动脉中α受体密度这一假说。