神经降压素的结构-抗伤害感受活性研究

Structure-antinociceptive activity studies with neurotensin.

作者信息

Furuta S, Kisara K, Sakurada S, Sakurada T, Sasaki Y, Suzuki K

出版信息

Br J Pharmacol. 1984 Sep;83(1):43-8. doi: 10.1111/j.1476-5381.1984.tb10117.x.

DOI:10.1111/j.1476-5381.1984.tb10117.x

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1987165/

Abstract

The antinociceptive effects of synthetic neurotensin (NT), its fragments and analogues administered into the lateral cerebroventricle have been compared in the conscious mouse. Intracerebroventricular (i.c.v.) administration of NT produced a dose-dependent antinociceptive effect in the tail pressure test. The NT fragments and analogues, NT(8-13), NT(8-10), NT(9-13), NT(9-11), NT(8-11) NHEt and NT(9-11) NHEt were also effective antinociceptive peptides. The potency of NT(8-13) and the duration of its effects were found to be approximately equal to those of NT. The antinociceptive effects produced by NT, NT(8-13) and NT(9-13) were significantly reversed by the opioid antagonist naloxone but not by thyrotropin releasing hormone. It is concluded that NT(8-13) is required for the full expression of the antinociceptive effects of NT which may be mediated in part through the brain opioid system.

摘要

在清醒小鼠中比较了侧脑室注射合成神经降压素（NT）、其片段及类似物的抗伤害感受作用。脑室内（i.c.v.）注射NT在尾压试验中产生剂量依赖性抗伤害感受作用。NT片段及类似物，即NT(8 - 13)、NT(8 - 10)、NT(9 - 13)、NT(9 - 11)、NT(8 - 11) NHEt和NT(9 - 11) NHEt也是有效的抗伤害感受肽。发现NT(8 - 13)的效力及其作用持续时间与NT大致相当。NT、NT(8 - 13)和NT(9 - 13)产生的抗伤害感受作用可被阿片类拮抗剂纳洛酮显著逆转，但不能被促甲状腺激素释放激素逆转。得出的结论是，NT(8 - 13)是NT抗伤害感受作用充分发挥所必需的，其抗伤害感受作用可能部分通过脑阿片系统介导。

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