Life sciences · 2005
Vasorelaxing effect of U50,488H in pulmonary artery and underlying mechanism in rats.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Sun Xin, Ma Sai, Zang Yi-Min, Lu Shun-Yan, Guo Hai-Tao, Bi Hui, Wang Yue-Min, Ma Heng, Ma Xin-Liang, Pei Jian-Ming
Аннотация
AIM: To investigate the relaxation effect and underlying mechanism of U50,488H (a selective kappa-opioid receptor agonist) in pulmonary artery in the rat.
METHODS: Isolated pulmonary artery ring was perfused and the tension of the vessel was measured.
RESULTS: U50,488H relaxed the pulmonary artery ring in a dose-dependent manner and the effect was abolished by nor-binaltorphimine, a selective kappa-opioid receptor antagonist. The relaxation effect of U50,488H in pulmonary artery was partially endothelium-dependent and was significantly attenuated in the presence of L-NAME. The relaxation effect of U50,488H was significantly attenuated by K(V) channel blocker 4-AP (4-aminopyridine), but not by glibenclamide (ATP-sensitive K+ channel blocker) nor TEA (tetraethylamonium, Ca2+-activated K+ channel blocker). Further study also showed that endothelium denudation and 4-AP have an additive inhibitory effect on pulmonary artery relaxation caused by U50,488H.
CONCLUSION: Kappa-opioid receptor activation by U50,488H relaxes pulmonary artery via two separate pathways: one is endothelium-derived nitric oxide, the other is K(V) channel in pulmonary artery smooth muscle.
METHODS: Isolated pulmonary artery ring was perfused and the tension of the vessel was measured.
RESULTS: U50,488H relaxed the pulmonary artery ring in a dose-dependent manner and the effect was abolished by nor-binaltorphimine, a selective kappa-opioid receptor antagonist. The relaxation effect of U50,488H in pulmonary artery was partially endothelium-dependent and was significantly attenuated in the presence of L-NAME. The relaxation effect of U50,488H was significantly attenuated by K(V) channel blocker 4-AP (4-aminopyridine), but not by glibenclamide (ATP-sensitive K+ channel blocker) nor TEA (tetraethylamonium, Ca2+-activated K+ channel blocker). Further study also showed that endothelium denudation and 4-AP have an additive inhibitory effect on pulmonary artery relaxation caused by U50,488H.
CONCLUSION: Kappa-opioid receptor activation by U50,488H relaxes pulmonary artery via two separate pathways: one is endothelium-derived nitric oxide, the other is K(V) channel in pulmonary artery smooth muscle.
Предметные рубрики MeSH
3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-IsomerAdrenergic beta-AntagonistsAnimalsAnti-Inflammatory Agents, Non-SteroidalAntihypertensive AgentsAtropineDynorphinsEndothelium, VascularEnzyme InhibitorsIn Vitro TechniquesIndomethacinMaleMuscle RelaxationMuscle, Smooth, VascularNG-Nitroarginine Methyl EsterNitric OxideNitric Oxide Synthase Type IIIPeptide FragmentsPotassium Channel BlockersPotassium ChannelsPropranololPulmonary ArteryRatsRats, Sprague-DawleyReceptors, Opioid, kappa