Oriowo M A, Bevan R D, Bevan J A
Department of Pharmacology, College of Medicine, University of Vermont, Burlington 05405.
Eur J Pharmacol. 1992 Jun 17;216(3):415-20. doi: 10.1016/0014-2999(92)90439-b.
Interaction with chlorethylclonidine has been used to subdivide populations of alpha 1-adrenoceptors in some tissues. WB 4101 can distinguish high and low affinity states of the receptor. The present study was carried out to determine if different populations or affinity states of alpha 1-adrenoceptors distinguished by either of these compounds, could explain the variation in alpha 1-adrenoceptor agonist affinity found amongst rabbit arteries. Five arteries were studied whose affinity for noradrenaline vary between 4.8 and 6.4. These were the thoracic aorta, renal, superior mesenteric, ear and ovarian arteries. WB 4101 was found to be equally effective in antagonizing noradrenaline on all arteries. Chlorethylclonidine caused a 20-fold rightward shift of the noradrenaline dose-contraction curve in the thoracic aorta; but had little or no effect on the other vessels. Thus, the combination of different proportions of subsets of alpha 1-adrenoceptors distinguished by WB 4101 or chlorethylclonidine does not explain the variation in alpha 1-adrenoceptor affinity found in these rabbit arteries.
在某些组织中,与氯乙可乐定的相互作用已被用于细分α1 -肾上腺素能受体群体。WB 4101可以区分该受体的高亲和力和低亲和力状态。进行本研究以确定通过这两种化合物之一区分的α1 -肾上腺素能受体的不同群体或亲和力状态,是否可以解释在兔动脉中发现的α1 -肾上腺素能受体激动剂亲和力的变化。研究了五条动脉,它们对去甲肾上腺素的亲和力在4.8至6.4之间变化。这些动脉分别是胸主动脉、肾动脉、肠系膜上动脉、耳动脉和卵巢动脉。发现WB 4101在拮抗所有动脉上的去甲肾上腺素方面同样有效。氯乙可乐定使胸主动脉中去甲肾上腺素剂量 - 收缩曲线向右移动20倍;但对其他血管几乎没有影响。因此,由WB 4101或氯乙可乐定区分的α1 -肾上腺素能受体亚群的不同比例组合,并不能解释在这些兔动脉中发现的α1 -肾上腺素能受体亲和力的变化。