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在麻醉大鼠中,由β-内啡肽、DAMGO和吗啡从延髓头端腹外侧网状核(ROb)和延髓腹外侧区(GiA)诱导甩尾抑制的不同机制。

Different mechanisms mediating tail-flick inhibition induced by beta-endorphin, DAMGO and morphine from ROb and GiA in anesthetized rats.

作者信息

Tseng L F, Collins K A

机构信息

Department of Pharmacology and Toxicology, Medical College of Wisconsin, Milwaukee.

出版信息

J Pharmacol Exp Ther. 1991 Apr;257(1):530-8.

PMID:2020008
Abstract

The effects of beta-endorphin, D-Ala2-NMePhe4-Gly-ol-enkephalin (DAMGO) and morphine microinjected into raphe obscurus nucleus (ROb) and gigantocellular reticular nucleus alpha (GiA) in inhibiting the tail-flick response were studied in pentobarbital anesthetized rats. beta-Endorphin (0.1-3 micrograms) microinjected into ROb inhibited the tail-flick response dose-dependently and produced 100% inhibition at high doses (greater than 3 micrograms). DAMGO [0.004-0.015 micrograms] injected into ROb, also dose-dependently, inhibited the tail-flick response but reached a plateau of 60 to 80% inhibition at high doses (greater than 0.015 micrograms). Morphine (10-60 micrograms) injected into ROb produced only a small inhibition (less than 20% inhibition) even at high doses (greater than 60 micrograms). The rank order of potency of these opioids on the tail-flick inhibition was DAMGO greater than beta-endorphin greater than morphine. Morphine (1-10 micrograms) and DAMGO (0.004-0.03 micrograms) microinjected into GiA produced dose-dependent inhibitions of the tail-flick response and high doses of these two mu agonists fully inhibited the tail-flick response. However, beta-endorphin (0.1-10 micrograms) injected into GiA produced a small but dose-dependent inhibition of the tail-flick response (less than 60% inhibition). The rank order of potency of these opioids on the tail-flick inhibition was DAMGO greater than beta-endorphin greater than morphine. The inhibition of the tail-flick response induced by beta-endorphin (2 micrograms) microinjected into ROb was blocked by the coadministration of beta-endorphin-[1-27] (6 micrograms), but not naloxone (1 microgram).(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在戊巴比妥麻醉的大鼠中,研究了微量注射到中缝隐核(ROb)和巨细胞网状核α(GiA)中的β-内啡肽、D-丙氨酸2-N-甲基苯丙氨酸4-甘氨醇脑啡肽(DAMGO)和吗啡对甩尾反应的抑制作用。微量注射到ROb中的β-内啡肽(0.1 - 3微克)剂量依赖性地抑制甩尾反应,高剂量(大于3微克)时产生100%抑制。注射到ROb中的DAMGO[0.004 - 0.015微克]也呈剂量依赖性地抑制甩尾反应,但高剂量(大于0.015微克)时达到60%至80%抑制的平台期。即使高剂量(大于60微克)注射到ROb中的吗啡(10 - 60微克)也仅产生小幅度抑制(小于20%抑制)。这些阿片类药物对甩尾抑制作用的效价顺序为DAMGO>β-内啡肽>吗啡。微量注射到GiA中的吗啡(1 - 10微克)和DAMGO(0.004 - 0.03微克)产生剂量依赖性的甩尾反应抑制,这两种μ激动剂的高剂量完全抑制甩尾反应。然而,注射到GiA中的β-内啡肽(0.1 - 10微克)产生小幅度但剂量依赖性的甩尾反应抑制(小于60%抑制)。这些阿片类药物对甩尾抑制作用的效价顺序为DAMGO>β-内啡肽>吗啡。微量注射到ROb中的β-内啡肽(2微克)诱导的甩尾反应抑制被同时给予的β-内啡肽-[1 - 27](6微克)阻断,但未被纳洛酮(1微克)阻断。(摘要截断于250字)

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