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目的:探索双苯氟嗪(Dip,一种我国自行合成的桂利嗪衍生物),对5-羟色胺所致的脑动脉收缩的影响。方法:比较双苯氟嗪、氟桂利嗪(Flu)、桂利嗪(Cin)对5-羟色胺所致离体猪基底动脉收缩的抑制及两种收缩成分的影响。结果:三者的拮抗作用强度顺序(IC_(50))为Dip 4.0μmol·L~(-1)>Flu15.6μmol·L~(-1)>Cin 25.2umo·L~(-1)。这三种药对5-羟色胺所致离体猪基底动脉的两种收缩成分均有拮抗。Dip和Cin抑制收缩的快速相强于持续相,而Flu对二者的作用无显著差异。结论:在Dip,Flu和Cin三种药之中,Dip对脑血管的扩张作用最强,其原因主要与抑制内钙的释放有关。
Objective: To explore the effect of Diphenhydramine on the contractions of cerebral arteries induced by 5-hydroxytryptamine. Methods: The effects of dipfluzine, flunarizine (Flu) and cinarin on contraction of isolated basilar artery induced by 5-hydroxytryptamine and the effects of two contractile components were compared. Results: The order of intensities of antagonism (IC 50) was Dip 4.0 μmol·L -1> Flu 15.6 μmol·L -1> Cin 25.2umo · L -1. These three drugs antagonize the two contractile components of isolated porcine basilar artery induced by 5-HT. Dip and Cin inhibit the contraction of the fast phase stronger than the continuous phase, while the Flu on the two no significant difference. Conclusion: Among the three drugs Dip, Flu and Cin, Dip has the strongest effect on the expansion of cerebrovascular. The reason is mainly related to the inhibition of the release of intracellular calcium.