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机构地区:[1]浙江大学医学院基础药理学教研室
出 处:《Acta Pharmacologica Sinica》2000年第10期84-87,共4页中国药理学报(英文版)
摘 要:AIM:To study the effect of nociceptin (orphanin FQ), a newly discovered heptadecapeptide, on cholinergic constrictions in isolated trachea and bronchus of rat. METHODS: The electric field stimulation (EPS) induced a monophasic constriction, which was due to an activation of the cholinergic nerves. RESULTS: Nociceptin 0.001 -0.1μmol/L inhibited cholinergic constriction in a concentration-dependent manner. IC50 (95 % of confidence limits) were 0.06 (0.04-0.08) μmol/L and 0.07 (0.05-0.1) μmol/L in tracheae and bronchi respectively. The constrictions inhibited by nociceptin 0.01 μmol/L in tracheae and bronchi were (58 +32) % and (60+ 26) % respectively compared with the control, in which nociceptin was not applied. After pretreatment with naloxone 0.1 μmol/L, the constrictions were (60+ 19) % and (54 + 20) % (P> 0.05 vs the above figures) . However, the constrictions induced by exogenous acetylcholine were unaffected by nociceptin 0.01 μmol/ L. k-Opioid receptor agonist, U-50488H (0.01-1 μmol/L) did not affect the EFS-induced cholinergic constrictions in rat airways. CONCLUSION: Nociceptin inhibits EFS-induced cholinergic constriction, which is not affected by naloxone in rat airways.目的:研究痛啡肽(nociceptin)对大鼠离体气管/支气管的胆碱能神经兴奋所致收缩的抑制作用.方法:记录电场刺激引起胆碱能神经兴奋所致的标本收缩张力,了解nociceptin的作用.结果:Nociceptin0.001-0.1μmol/L可抑制标本的胆碱能收缩,其IC_(50)(95%的可信限)分别是0.06(0.04-0.08)μmol/L和0.07(0.05-0.1)μmol/L.在气管和支气管上,nociceptin 0.01μmol/L的抑制率分别是:(58±32)%和(60±26)%;预用纳洛酮0.1μmol/L后,nociceptin的抑制率为:(60±19)%和(54±20)%(P>0.05).Nociceptin 0.01μmol/L不影响外源性乙酰胆碱引起的气道标本收缩.κ阿片受体激动剂U-50488H 0.01—1 μmol/L不影响电场刺激引起的大鼠气道胆碱能收缩.结论:痛啡肽抑制电刺激引起的大鼠气道胆碱能收缩反应,且不受纳洛酮影响.
关 键 词:NOCICEPTIN kappa opioid receptors TRACHEA BRONCHI electric stimulation cholinergic fibers
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