EndothelinB (ETB) receptor-activated potentiation of cholinergic nerve-mediated contraction in human bronchus.
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.
Fernandes
L B
LB
Department of Pharmacology, University of Western Australia, Nedlands, Australia.
Henry
P J
PJ
Rigby
P J
PJ
Goldie
R G
RG
D000368:Aged; D001980:Bronchi / Q000187:drug effects*; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009119:Muscle Contraction / Q000187:drug effects*; D009842:Oligopeptides / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D017466:Receptors, Endothelin / Q000187:drug effects*; D013779:Tetrodotoxin / Q000494:pharmacology; D014662:Vasoconstrictor Agents / Q000494:pharmacology; D014757:Viper Venoms / Q000494:pharmacology
D009842:Oligopeptides; D010880:Piperidines; D017466:Receptors, Endothelin; D014662:Vasoconstrictor Agents; D014757:Viper Venoms; C057354:sarafotoxins s6; D013779:Tetrodotoxin; C086539:BQ 788