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地西泮通过作用于2型苯二氮䓬受体来逆转戊四氮对幼鼠的影响。

Diazepam reverses the effects of pentylenetetrazole in rat pups by acting at type 2 benzodiazepine receptors.

作者信息

Johnston A L, File S E, Dingemanse J, Aranko K

机构信息

MRC Neuropharmacology Research Group, School of Pharmacy, University of London.

出版信息

Pharmacol Biochem Behav. 1989 Mar;32(3):823-5. doi: 10.1016/0091-3057(89)90041-5.

Abstract

Pentylenetetrazole (75 mg/kg) induced a characteristic coarse body tremor (accompanied by limb extension) and hyperactivity in 4-day-old rat pups. These effects were reversed by diazepam (0.5 and 2 mg/kg) but not by CL 218,872 (10 and 20 mg/kg) which is selective for type 1 benzodiazepine receptors. Diazepam did not affect the brain concentrations of pentylenetrazole, indicating that the reversal was not based on a pharmacokinetic interaction. Neither diazepam nor CL 218,872 had significant effects on the behavior of the rat pups, although diazepam (2 mg/kg) tended to increase locomotor activity. The results suggest that diazepam displays an anticonvulsant effect in the neonatal rat which is mediated by type 2 receptors.

摘要

戊四氮(75毫克/千克)可使4日龄大鼠幼崽出现典型的粗大身体震颤(伴有肢体伸展)和多动。地西泮(0.5和2毫克/千克)可逆转这些效应,但对1型苯二氮䓬受体具有选择性的CL 218,872(10和20毫克/千克)则不能。地西泮不影响戊四氮的脑内浓度,表明这种逆转并非基于药代动力学相互作用。尽管地西泮(2毫克/千克)倾向于增加运动活性,但地西泮和CL 218,872对大鼠幼崽的行为均无显著影响。结果表明,地西泮在新生大鼠中表现出由2型受体介导的抗惊厥作用。

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