内皮素ETA和ETB受体介导血管平滑肌收缩。
Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction.
作者信息
Sumner M J, Cannon T R, Mundin J W, White D G, Watts I S
机构信息
Department of Cardiovascular and Respiratory Pharmacology, Glaxo Group Research Ltd., Ware, Herts.
出版信息
Br J Pharmacol. 1992 Nov;107(3):858-60. doi: 10.1111/j.1476-5381.1992.tb14537.x.
Abstract
- We have investigated the receptors mediating endothelin-induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA). 2. Endothelin-1 (ET-1) and endothelin-3 (ET-3) contracted RJV preparations with similar potency (EC50 values approximately 1 nM), whereas, ET-1 (EC50:4.5 nM) was approximately 80 fold more potent than ET-3 in contracting RTA. In addition, the ETB receptor-selective agonist [Ala1,3,11,15]ET-1 contracted RJV (EC50:2.1 nM) but not RTA. 3. The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET-1, but had no effect (at 10 microM) on the contractile effects of either ET-1, ET-3 or [Ala1,3,11,15]ET-1 in RJV. 4. These data suggest that both ETA and ETB receptors can mediate vascular smooth muscle contraction.
摘要
- 我们研究了介导内皮素诱导家兔离体颈静脉（RJV）和大鼠离体胸主动脉（RTA）收缩的受体。2. 内皮素-1（ET-1）和内皮素-3（ET-3）使RJV制剂收缩的效力相似（半数有效浓度[EC50]值约为1 nM），而ET-1（EC50：4.5 nM）在使RTA收缩方面的效力比ET-3高约80倍。此外，ETB受体选择性激动剂[Ala1,3,11,15]ET-1使RJV收缩（EC50：2.1 nM），但不使RTA收缩。3. ETA受体拮抗剂BQ123竞争性拮抗（pA2 6.93）ET-1引起的RTA收缩，但对RJV中ET-1、ET-3或[Ala1,3,11,15]ET-1的收缩作用（在10 microM时）无影响。4. 这些数据表明ETA和ETB受体均可介导血管平滑肌收缩。
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