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机构地区:[1]山西医学院药理教研室
出 处:《中国药理学与毒理学杂志》1994年第4期260-264,共5页Chinese Journal of Pharmacology and Toxicology
摘 要:本文比较性研究甲基黄酮醇胺盐酸盐(MFA),三氟拉嗪(Tri),维拉帕米(Ver),氨茶碱(Ami)和异丙肾上腺素(Iso)对豚鼠离体气管的舒张作用.MFA(0.1-0.3mmol·L-1)时间依赖性舒张KCl诱导的气管平滑肌收缩。低于0.1mmol·L-1时MFA对KCl诱导的收缩仅有轻微作用,却使Iso和Ami的浓度舒张曲线明显向左上移动。MFA,Ver,Tri使CaCl2量效曲线向右下移,pD2值分别为:5.0±s0.5,6.4±s0.8,5.0±s0.6.MFA,Ver,Tri,Ami剂量依赖性抑制次大量生理激动剂所致的收缩,其作用强度顺序为:Tri>Ver=MFA>Ami.提示MFA具有非竞争性钙拮抗作用,其作用方式与Tri相似。与Ami相比、MFA是一个较强的主气管扩张剂,并与Ami,Iso具有明显的协同舒张支气管作用。The effects of methylflavonolamine(MFA) on bronchoactive agents-induced contractionsand bronchodilators-induced relaxations were studiedon guinea-pig isolated trachea and compared withthat of verapamil (Ver) and trifluoperazine (Tri). At0.1-0.3 mmol · L-1, MFA timedependently relaxedthe contraction induced by 40 mmol · L 1 KCl. Atconcentration below 0. 1 mmol · L -1 , MFA produced anegligible relaxation on KCl-induced contraction, butsignificantly shifted the isoprenaline (lso) andaminophylline (Ami) concentration-relaxation curvesupwards to the left. MFA. Ver, Tri and Ami inhibitedthe contractions induced by submaximal concentra-tions of physiologic agonists. The inhibitory potencyorder was Tri> Ver = MFA > Ami. MFA. Ver and Trishifted CaCl2 cumulative curves downwards to theright with the pDz values 5.0± s 0.5, 6.4± s 0.8 and5.0± s 0.6, respectively. The present results show thatMFA is relatively potent to antagonize physiologicbronchoconstrictors and have synergistic action withIso and Ami in bronchodilation. It is also suggestedthat MFA may have non-selective calcium antagonis-tic action and resemble Tri more closely than Ver orAmi in the mechanism of action.
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