Fernandes L B, Henry P J, Rigby P J, Goldie R G
Department of Pharmacology, University of Western Australia, Nedlands, Australia.
Br J Pharmacol. 1996 Aug;118(8):1873-4. doi: 10.1111/j.1476-5381.1996.tb15617.x.
In human isolated bronchial preparations, the endothelinB (ETB) receptor-selective agonist, sarafotoxin S6c (Stx6c; 1 nM) increased nerve-mediated contraction in response to electrical field stimulation (EFS) at 0.5-1 Hz from 19 +/- 4% to 42 +/- 7% (n = 9). This effect was blocked in the presence of the ETB receptor-selective antagonist, BQ-788 (10 microM). These data are consistent with findings in some animal species that ET-1 and related peptides have marked neuromodulatory influences on the cholinergic system. Furthermore, they provide additional support for the concept that ET-1 may have a mediator role in bronchial obstruction in asthma.
在人离体支气管标本中,内皮素B(ETB)受体选择性激动剂,铃蟾毒素S6c(Stx6c;1 nM)可使电场刺激(EFS)频率为0.5 - 1 Hz时神经介导的收缩反应从19±4%增加至42±7%(n = 9)。在ETB受体选择性拮抗剂BQ - 788(10 μM)存在的情况下,该效应被阻断。这些数据与在一些动物物种中的发现一致,即内皮素 - 1(ET - 1)及相关肽对胆碱能系统具有显著的神经调节作用。此外,它们为ET - 1可能在哮喘支气管阻塞中起介质作用这一概念提供了更多支持。