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一种阿片肽降解抑制剂在小鼠中产生镇痛作用。

An inhibitor of opioid peptide degradation produces analgesia in mice.

作者信息

Simmons W H, Ritzmann R F

出版信息

Pharmacol Biochem Behav. 1980 Nov;13(5):715-8. doi: 10.1016/0091-3057(80)90016-7.

Abstract

Bacitracin, a known inhibitor of brain peptidases which degrade the enkephalins and endorphins, produced dose-dependent analgesia in mice when injected into the lateral ventricle of the brain as determined by the tail-flick assay. The analgesic response peaked at 15 min post-injection but was reduced to control levels by 3.5 hours. Naloxone reversed the analgesic response to bacitracin, suggesting that opiate receptors may be involved. It is proposed that bacitracin produces analgesia by preventing the enzymatic destruction of endogenously released opioid peptides.

摘要

杆菌肽是一种已知的脑肽酶抑制剂,可降解脑啡肽和内啡肽。通过甩尾试验测定,当将其注射到小鼠脑侧脑室时,会产生剂量依赖性镇痛作用。镇痛反应在注射后15分钟达到峰值,但在3.5小时后降至对照水平。纳洛酮可逆转对杆菌肽的镇痛反应,提示可能涉及阿片受体。有人提出,杆菌肽通过防止内源性释放的阿片肽被酶破坏而产生镇痛作用。

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