Inhibitory effects of putative peptidic urotensin-II receptor antagonists on urotensin-II-induced contraction of cat isolated respiratory smooth muscle
European Journal of Pharmacology(2005)
摘要
Urotensin-II is purported to influence pulmonary function by modulating smooth muscle tone/growth. In the present study, Northern blot and reverse transcription polymerase chain reaction (RT-PCR) analysis indicated the presence of UT receptor mRNA in cat trachea, bronchi and lung parenchyma. Urotensin-II contracted cat isolated trachea and bronchi with similar potencies (pEC50s 8.61±0.07–8.81±0.10). Contractile efficacies ranged from 19±9% to 63±11% KCl in the primary and secondary bronchi. The peptidic UT receptor antagonists BIM-23127, SB-710411 and GSK248451 (7.18±0.12, 7.52±0.08 and 9.05±0.16 cat recombinant UT pKis) inhibited urotensin-II-induced contraction of cat isolated trachea with pKbs 6.36±0.11, 6.74±0.07 and 9.27±0.12, respectively. As such, feline lung contains significant amounts of UT mRNA and this receptor appears to be functionally coupled to bronchoconstriction (the peptidic tool compound GSK248451 representing a sub-nanomolar inhibitor of such effects). These findings suggest that the cat represents a suitable species for future studies designed to assess the effects of the urotensin-II receptor on pulmonary (patho)physiology.
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关键词
Urotensin-II,GPR14,UT receptor,BIM-23127,SB-710411,GSK248451,Trachea,Bronchus
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