非儿茶酚型苯乙胺衍生物诱导的抗伤害感受特性：内源性去甲肾上腺素与苯乙胺类似物诱导的抗伤害感受之间的关系。

Characteristics of antinociception induced by noncatecholic phenylethylamine derivatives: the relation of endogenous norepinephrine to phenylethylamine analog-induced antinociception.

作者信息

Matsuoka Y, Sakuma M, Sugioka T, Terawaki Y, Uruno T, Kubota K

机构信息

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.

出版信息

Jpn J Pharmacol. 1988 Oct;48(2):263-72. doi: 10.1254/jjp.48.263.

DOI:10.1254/jjp.48.263

PMID:3210449

Abstract

Characteristics of the antinociceptive action of phenylethylamine derivatives, amphetamine, beta-phenylethylamine (PEA) and beta-hydroxyphenylethylamine (OHPEA), were examined. The pain threshold of mice was measured by using the hot plate method. Intraperitoneal administration of alpha-methyl-p-tyrosine inhibited antinociception induced by PEA and OHPEA, and intracisternal administration of norepinephrine increased antinociception induced by PEA and OHPEA. Intracisternal administration of phentolamine inhibited the antinociception induced by PEA derivatives. The levels of norepinephrine and normetanephrine in the brain were determined by using HPLC. PEA derivatives decreased norepinephrine in the brain and tended to increase normetanephrine at 15 min after the administration of PEA derivatives. These findings indicate that PEA derivatives cause the release of norepinephrine in the central nervous system, and the released norepinephrine induces antinociception.

摘要

研究了苯乙胺衍生物、苯丙胺、β-苯乙胺（PEA）和β-羟基苯乙胺（OHPEA）的抗伤害感受作用特性。采用热板法测量小鼠的痛阈。腹腔注射α-甲基对酪氨酸可抑制PEA和OHPEA诱导的抗伤害感受，脑池内注射去甲肾上腺素可增强PEA和OHPEA诱导的抗伤害感受。脑池内注射酚妥拉明可抑制PEA衍生物诱导的抗伤害感受。采用高效液相色谱法测定脑中去甲肾上腺素和去甲变肾上腺素的水平。PEA衍生物给药后15分钟，可降低脑中去甲肾上腺素水平，并倾向于增加去甲变肾上腺素水平。这些发现表明，PEA衍生物可导致中枢神经系统中去甲肾上腺素的释放，而释放的去甲肾上腺素可诱导抗伤害感受。