神经降压素对大鼠蓝斑核中芬太尼诱导的肌肉强直的拮抗作用。

Antagonization of fentanyl-induced muscular rigidity by neurotensin at the locus coeruleus of the rat.

作者信息

Wang S W, Tsou M Y, Lee T Y, Chan S H, Lui P W

机构信息

Institute of Pharmacology, National Yang-Ming Medical College, Veterans General Hospital-Taipei, Taiwan, ROC.

出版信息

Regul Pept. 1994 Apr 14;51(1):33-40. doi: 10.1016/0167-0115(94)90132-5.

DOI:10.1016/0167-0115(94)90132-5

PMID:8036282

Abstract

We evaluated the interaction between neurotensin (NT) and mu-opioid receptors at the locus coeruleus (LC), using fentanyl-induced muscular rigidity as our experimental index. Adult, male Sprague-Dawley rats anesthetized with ketamine (120 mg/kg, i.p., with 24 mg/kg/h i.v. infusion supplements) were used. Intravenous injection of fentanyl (100 micrograms/kg) consistently promoted a significant increase in the electromyographic activity recorded from the sacrococcygeus dorsalis lateralis muscle. This implied muscular rigidity was appreciably and dose-dependently antagonized by prior intracerebroventricular (i.c.v.) application of NT (15, 30 or 60 nmol/5 microliter). Microinjection of the tridecapeptide (300 or 600 pmol/100 nl) into the bilateral LC produced similar results. This suppressive effect of NT on fentanyl-induced muscular rigidity was antagonized by simultaneously administered NT antiserum (1:80), or partially blocked by its antagonist, (D-Trp11)-NT (300 pmol), but not by normal rabbit serum (1:80). These results suggest that NT may interact with the mu-opioid receptors at the LC, resulting in the suppression of fentanyl-induced muscular rigidity in the rat.

摘要

我们以芬太尼诱导的肌肉强直作为实验指标，评估了蓝斑（LC）处神经降压素（NT）与μ-阿片受体之间的相互作用。使用成年雄性Sprague-Dawley大鼠，用氯胺酮（120 mg/kg，腹腔注射，静脉输注补充剂为24 mg/kg/h）麻醉。静脉注射芬太尼（100微克/千克）持续促进从骶尾背外侧肌记录的肌电图活动显著增加。这表明预先脑室内（i.c.v.）应用NT（15、30或60 nmol/5微升）可明显且剂量依赖性地拮抗这种肌肉强直。向双侧LC微量注射十三肽（300或600 pmol/100 nl）产生了类似的结果。NT对芬太尼诱导的肌肉强直的这种抑制作用被同时给予的NT抗血清（1:80）拮抗，或被其拮抗剂（D-Trp11）-NT（300 pmol）部分阻断，但未被正常兔血清（1:80）阻断。这些结果表明，NT可能在LC处与μ-阿片受体相互作用，从而抑制大鼠中芬太尼诱导的肌肉强直。