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丙谷胺可预防和减轻大鼠对吗啡的急性耐受性。

Proglumide prevents and curtails acute tolerance to morphine in rats.

作者信息

Tang J, Chou J, Iadarola M, Yang H Y, Costa E

出版信息

Neuropharmacology. 1984 Jun;23(6):715-8. doi: 10.1016/0028-3908(84)90171-0.

DOI:10.1016/0028-3908(84)90171-0
PMID:6462377
Abstract

The antagonism of the antinociceptive action of morphine elicited by CCK-8-SO4 can be counteracted by proglumide, a CCK antagonist. The addition of morphine (10(-6)M) to the artificial spinal fluid perfusing the subarachnoidal space of rat spinal cord increases the CCK content of the perfusate. Proglumide can potentiate morphine analgesia without changing the half life of morphine. After seven to eight subcutaneous injections of morphine (4 mg/kg) repeated every two hrs there is tolerance to the antinociceptive action of morphine. Proglumide can partially block or reverse this acute tolerance to morphine.

摘要

CCK - 8 - SO4引发的对吗啡镇痛作用的拮抗可被CCK拮抗剂丙谷胺抵消。向灌注大鼠脊髓蛛网膜下腔的人工脑脊液中添加吗啡(10⁻⁶M)可增加灌注液中的CCK含量。丙谷胺可增强吗啡镇痛作用,而不改变吗啡的半衰期。每两小时皮下注射七至八次吗啡(4毫克/千克)后,会出现对吗啡镇痛作用的耐受性。丙谷胺可部分阻断或逆转这种对吗啡的急性耐受性。

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