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氯胺酮光学异构体在小鼠体内的比较药理学

Comparative pharmacology of the optical isomers of ketamine in mice.

作者信息

Ryder S, Way W L, Trevor A J

出版信息

Eur J Pharmacol. 1978 May 1;49(1):15-23. doi: 10.1016/0014-2999(78)90217-0.

Abstract

Relative pharmacological potencies of the optical isomers of ketamine have been estimated in ICR mice. The (+)-isomer was 3X more potent than (-)-ketamine as an analgesic using the phenylquinone writhing test, only 1.5X more potent in terms of hypnotic activity and 1.8X more potent in causing locomotor stimulation. At equianalgesic doses (+)-ketamine caused less stimulation of locomotor activity than the (-)-isomer. These potency differences did not appear to be due to differences in biodisposition although stereoselective metabolism was demonstrated in vivo. Analgesia induced by ketamine was reversed by 10 mg/kg of naloxone.

摘要

已在ICR小鼠中评估了氯胺酮光学异构体的相对药理效价。使用苯醌扭体试验时,(+)-异构体作为镇痛药的效力比(-)-氯胺酮强3倍,就催眠活性而言仅强1.5倍,在引起运动刺激方面强1.8倍。在等效镇痛剂量下,(+)-氯胺酮引起的运动活动刺激比(-)-异构体少。尽管在体内证明了立体选择性代谢,但这些效价差异似乎并非由于生物处置的差异所致。10mg/kg的纳洛酮可逆转氯胺酮诱导的镇痛作用。

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