Moreland S, McMullen D M, Delaney C L, Lee V G, Hunt J T
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08540-4000.
Biochem Biophys Res Commun. 1992 Apr 15;184(1):100-6. doi: 10.1016/0006-291x(92)91163-k.
Two endothelin (ET) receptor subtypes have been identified to date: the ETA receptor which preferentially binds ET-1 over ET-3, and the ETB receptor which is non-selective. This study characterized the ET receptor subtypes present in several vascular smooth muscle preparations using standard in vitro techniques. In all but one of the arteries tested, ET-3 was significantly less potent than ET-1. In contrast, the potency of ET-3 was very similar to that of ET-1 in all of the veins. The selective ETA receptor antagonist BQ-123 blunted the ET-1 contractions in rabbit carotid artery, but not in saphenous vein. The selective ETB receptor ligand sarafotoxin S6c contracted the rabbit saphenous vein, but not the carotid artery. These data suggest that vascular smooth muscle cells express ETA and ETB receptors. Stimulation of either receptor subtype can result in force development.
迄今为止,已鉴定出两种内皮素(ET)受体亚型:ETA受体优先结合ET-1而非ET-3,以及无选择性的ETB受体。本研究使用标准体外技术对几种血管平滑肌制剂中存在的ET受体亚型进行了表征。在所有测试的动脉中,除了一条动脉外,ET-3的效力明显低于ET-1。相比之下,ET-3在所有静脉中的效力与ET-1非常相似。选择性ETA受体拮抗剂BQ-123减弱了兔颈动脉中ET-1的收缩作用,但在隐静脉中则没有。选择性ETB受体配体沙拉毒素S6c使兔隐静脉收缩,但不使颈动脉收缩。这些数据表明血管平滑肌细胞表达ETA和ETB受体。刺激任何一种受体亚型均可导致肌力增加。