Takayanagi I, Harada M, Koike K, Satoh M
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Can J Physiol Pharmacol. 1991 Dec;69(12):1819-24. doi: 10.1139/y91-269.
Based on affinity for WB4101 and susceptibility to chloroethylclonidine, we evaluated the subtype of alpha 1-adrenoceptors activated by phenylephrine (a full agonist) and tizanidine (a partial agonist). The rabbit thoracic aorta and common iliac artery contain both alpha 1A- and alpha 1B-adrenoceptors, but the alpha 1B-subtype may be more predominantly in the common iliac artery than in the thoracic aorta. In rabbit thoracic aorta and common iliac artery, phenylephrine induced contraction through both alpha 1A- and alpha 1B-subtypes and tizanidine through only the alpha 1A-subtype. The subtype activated by phenylephrine may be partly different from that activated by tizanidine in the preparations used herein.
基于对WB4101的亲和力和对氯乙可乐定的敏感性,我们评估了由去氧肾上腺素(一种完全激动剂)和替扎尼定(一种部分激动剂)激活的α1-肾上腺素能受体亚型。兔胸主动脉和髂总动脉同时含有α1A-和α1B-肾上腺素能受体,但α1B亚型在髂总动脉中可能比在胸主动脉中更占优势。在兔胸主动脉和髂总动脉中,去氧肾上腺素通过α1A-和α1B-亚型诱导收缩,而替扎尼定仅通过α1A-亚型诱导收缩。在此所用的制剂中,去氧肾上腺素激活的亚型可能与替扎尼定激活的亚型部分不同。