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异氟磷噻平对映体对大鼠催乳素分泌及断头后惊厥的影响。

Effects of isofloxythepin enantiomers on prolactin secretion and postdecapitation convulsions in rats.

作者信息

Matsuo N, Yamada K, Matsumoto S, Domae M, Shirakawa K, Furukawa T

机构信息

Department of Pharmacology, School of Medicine, Fukuoka University, Japan.

出版信息

Pharmacol Biochem Behav. 1988 Aug;30(4):1081-3. doi: 10.1016/0091-3057(88)90143-8.

Abstract

Racemic isofloxythepin and its enantiomers (0.05-1.0 mg/kg) administered subcutaneously increased serum prolactin levels in a dose-dependent manner in rats. The potencies of the drugs were equal for this variable. They (0.05-1.0 mg/kg, SC) also decreased dose-dependently the incidence and duration of postdecapitation convulsions, the convulsions being abolished at 1.0 mg/kg in all groups. Although (-)-enantiomer had slightly stronger effects than those of raceme and (+)-enantiomer, there were no great differences in their inhibitory effects on postdecapitation convulsions. The results indicate that isofloxythepin enantiomers in addition to raceme increase serum prolactin levels and inhibit postdecapitation convulsions and that they seem to have similar potency in blocking of dopamine receptors and alpha 1-adrenoceptors.

摘要

消旋异氟西平及其对映体(0.05 - 1.0毫克/千克)皮下给药后,大鼠血清催乳素水平呈剂量依赖性升高。就这一变量而言,药物的效力相同。它们(0.05 - 1.0毫克/千克,皮下注射)还剂量依赖性地降低了断头后惊厥的发生率和持续时间,在所有组中,1.0毫克/千克时惊厥被消除。虽然(-)-对映体的作用比消旋体和(+)-对映体略强,但它们对断头后惊厥的抑制作用没有很大差异。结果表明,除消旋体外,异氟西平对映体也能提高血清催乳素水平并抑制断头后惊厥,并且它们在阻断多巴胺受体和α1 - 肾上腺素受体方面似乎具有相似的效力。

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