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甲基和苯基-3-甲氧基-4-羟基苯乙烯基酮的药理作用及急性毒性

Pharmacological actions and acute toxicity of methyl- and phenyl-3-methoxy-4-hydroxy styryl ketones.

作者信息

Singh G B, Leach G D, Atal C K

机构信息

Discipline of Pharmacology, Regional Research Laboratory, Jammu Tawi, India.

出版信息

Arzneimittelforschung. 1987 Jun;37(6):708-12.

PMID:3663269
Abstract

Some pharmacological actions and acute toxicity effects of methyl- and phenyl-3-methoxy-4-hydroxy styryl ketones have been described in experimental animals. The compounds antagonised the contractions evoked by a variety of agonists on several smooth muscle preparations in vitro. They produced inhibitory effects on spontaneously contracting uteri from pregnant rats and relaxant effects on pendular movements of rabbit duodenum and on dog intestinal movements in vivo. The compounds inhibited the castor oil induced diarrhoea in rat and propulsion of charcoal test meal in mice. Phenylbutazone showed similar effect on castor oil diarrhoea. The compounds failed to modify gestation period or parturition in pregnant rats. They antagonised bradykinin-induced bronchospasm in guinea pig. The compounds showed no significant effect on cardiovascular and respiratory systems: CNS and general behaviour were not affected even at high doses. Oral LD50 for both the compounds was greater than 2 g/kg.

摘要

甲基和苯基-3-甲氧基-4-羟基苯乙烯基酮的一些药理作用及急性毒性效应已在实验动物中得到描述。这些化合物在体外能拮抗多种激动剂对几种平滑肌制剂引起的收缩。它们对妊娠大鼠自发收缩的子宫产生抑制作用,对兔十二指肠的摆动运动以及对犬体内肠道运动产生松弛作用。这些化合物能抑制蓖麻油诱导的大鼠腹泻以及小鼠中炭末试验餐的推进。保泰松对蓖麻油腹泻有类似作用。这些化合物未能改变妊娠大鼠的妊娠期或分娩。它们能拮抗豚鼠中缓激肽诱导的支气管痉挛。这些化合物对心血管和呼吸系统无显著影响:即使在高剂量下,中枢神经系统和一般行为也未受影响。两种化合物的口服半数致死量均大于2克/千克。

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