The enhancing effects of peptidase inhibitors on the antinociceptive action of [Met5]enkephalin-Arg6-Phe7 in rats.

The enhancing effects of peptidase inhibitors on the antinociceptive action of [Met5]enkephalin-Arg6-Phe7 in rats. Research Abstract Details 

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The enhancing effects of peptidase inhibitors on the antinociceptive action of [Met5]enkephalin-Arg6-Phe7 in rats. Abstract Text:

Shigeru Takahashi,Xing Lu Jin,Kenya Kosaka,Masanobu Yoshikawa,Hiroyuki Kobayashi,Tetsuo Oka,Shigeru Takahashi,Xing Lu Jin,Kenya Kosaka,Masanobu Yoshikawa,Hiroyuki Kobayashi,Tetsuo Oka,

Previous in vitro studies have shown that the degradation of [Met(5)]enkephalin-Arg(6)-Phe(7) during incubation with cerebral membrane preparations is largely prevented by a mixture of three peptidase inhibitors: amastatin, captopril, and phosphoramidon. The present in vivo study shows that the inhibitory effect of [Met(5)]enkephalin-Arg(6)-Phe(7) administered intra-third-ventricularly on the tail-flick response was increased more than 1000-fold by the intra-third-ventricular pretreatment with three peptidase inhibitors. The antinociceptive effect produced by the [Met(5)]enkephalin-Arg(6)-Phe(7) in rats pretreated with any combination of two peptidase inhibitors was significantly smaller than that in rats pretreated with three peptidase inhibitors, indicating that any residual single peptidase could inactivate significant amounts of the [Met(5)]enkephalin-Arg(6)-Phe(7). The present data, together with those obtained from previous studies, clearly show that amastatin-, captopril-, and phosphoramidon-sensitive enzymes play important roles in the inactivation of endogenous opioid peptides, such as [Met(5)]enkephalin, [Met(5)]enkephalin-Arg(6)-Phe(7), [Met(5)]enkephalin-Arg(6)-Gly(7)-Leu(8), and dynorphin A (1-8), administered intra-third-ventricularly to rats.

The enhancing effects of peptidase inhibitors on the antinociceptive action of [Met5]enkephalin-Arg6-Phe7 in rats. Publishing Authors By Initials

S Takahashi,XL Jin,K Kosaka,M Yoshikawa,H Kobayashi,T Oka,S Takahashi,XL Jin,K Kosaka,M Yoshikawa,H Kobayashi,T Oka,

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The enhancing effects of peptidase inhibitors on the antinociceptive action of [Met5]enkephalin-Arg6-Phe7 in rats. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of pharmacological sciences

VOLUME: 105

Page Numbers: 117-21

Journal Abbreviation: J. Pharmacol. Sci.

ISSN: 1347-8613

DAY: 12

MONTH: 09

YEAR: 2007

The enhancing effects of peptidase inhibitors on the antinociceptive action of [Met5]enkephalin-Arg6-Phe7 in rats. Information

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LANGUAGE: eng

NlmUniqueID: 101167001

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AFFILIATION: Department of Clinical Pharmacology, School of Medicine, Tokai University, Isehara 259-1193, Japan.

Country: Japan

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MEDLINETA: J Pharmacol Sci

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