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一种新分离出的解痉剂——丁烯基苯酞。

A newly isolated antispasmodic--butylidenephthalide.

作者信息

Ko W C

出版信息

Jpn J Pharmacol. 1980 Feb;30(1):85-91. doi: 10.1254/jjp.30.85.

Abstract

Butylidenephthalide (BdPh), ligustilide and butylphthalide were isolated and purified from neutral oil of Ligusticum wallichii Franch. Among these three, BdPh proved to be the most active in inhibiting rat uterine contractions induced by prostaglandin F2 alpha, oxytocin and ACh. In studies done to compare the effects of BdPh and papaverine (Pap), guinea pig ileum, vas deferens and taenia coli were used. BdPh inhibited contractile responses of the ileum to agonists including ACh, K+ and Ba2+ in normal Tyrode solution and to exogenous Ca2+ in high K+ (80 mM), Ca2+-free Tyrode solution, and also responses of vas deferens responses to norepinephrine. Thus, BdPh is a non-specific antispasmodic but weaker in potency than Pap. However, as the inhibitory effects of BdPh on phasic contraction (PC) and tonic contraction (TC) of preparations, including depolarized and non-depolarized ileum and taenia coli, were much the same, it is suggested that the action mechanism of BdPh may differ from that of Pap which inhibited TC more selectively than PC. It may be concluded that BdPh possesses an non-specific antispasmodic action like Pap, the mechanism of action being different from that of Pap.

摘要

从川芎的中性油中分离并纯化出丁烯基苯酞(BdPh)、藁本内酯和丁基苯酞。在这三种物质中,BdPh在抑制前列腺素F2α、催产素和乙酰胆碱诱导的大鼠子宫收缩方面表现出最强的活性。在比较BdPh和罂粟碱(Pap)作用效果的研究中,使用了豚鼠回肠、输精管和结肠带。BdPh在正常台氏液中抑制回肠对包括乙酰胆碱、K+和Ba2+在内的激动剂的收缩反应,以及在高K+(80 mM)、无Ca2+的台氏液中对外源Ca2+的收缩反应,还抑制输精管对去甲肾上腺素的反应。因此,BdPh是一种非特异性解痉剂,但效力比Pap弱。然而,由于BdPh对包括去极化和未去极化的回肠和结肠带在内的标本的相性收缩(PC)和张力性收缩(TC)的抑制作用大致相同,提示BdPh的作用机制可能与Pap不同,Pap对TC的抑制比对PC更具选择性。可以得出结论,BdPh具有与Pap类似的非特异性解痉作用,但其作用机制与Pap不同。

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