Comparative antagonism by naltrexone and naloxone of μ, κ, and δ agonists

A. E. Takemori; P. S. Portoghese

doi:10.1016/0014-2999(84)90374-1

Comparative antagonism by naltrexone and naloxone of μ, κ, and δ agonists

A. E. Takemori, P. S. Portoghese

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

61 Scopus citations

Abstract

In the guinea pig ileum preparation, naltrexone was 3.5 to 5 times more potent than naloxone in antagonizing morphine but the antagonists were equipotent in antagonizing ethylketazocine. In the mouse vas deferens preparation, naltrexone and naloxone were equipotent in antagonizing both morphine and [D-Ala²-D-Leu⁵]enkephalin. The data provide evidence that the naltrexone-reversible μ population of receptors in the guinea pig ileum are different from those in the mouse vas deferens. These findings also point out the uniqueness of the μ receptor system in the guinea pig ileum which is reflected by the potency differences between naltrexone and naloxone.

Original language	English (US)
Pages (from-to)	101-104
Number of pages	4
Journal	European Journal of Pharmacology
Volume	104
Issue number	1-2
DOIs	https://doi.org/10.1016/0014-2999(84)90374-1
State	Published - Sep 3 1984

Bibliographical note

Funding Information:
In most of the above studies the antagonistic activity of naltrexone was tested principally against morphine, a prototypical tt-opioid agonist. In this study, we have used the guinea pig ileum and mouse vas deferens preparations and the concept * This work was supported by U.S. Public Health Grants from the National Institute on Drug Abuse. t To whom all correspondence should be addressed: Depart-ment of Pharmacology, 3-260 Millard Hall, University of Minnesota, 435 Delaware Street S.E., Minneapolis, MN 55455, U.S.A.

Keywords

Agonist
Antagonist
Naloxone
Naltrexone
Opioid
Receptor type

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10.1016/0014-2999(84)90374-1

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title = "Comparative antagonism by naltrexone and naloxone of μ, κ, and δ agonists",

abstract = "In the guinea pig ileum preparation, naltrexone was 3.5 to 5 times more potent than naloxone in antagonizing morphine but the antagonists were equipotent in antagonizing ethylketazocine. In the mouse vas deferens preparation, naltrexone and naloxone were equipotent in antagonizing both morphine and [D-Ala2-D-Leu5]enkephalin. The data provide evidence that the naltrexone-reversible μ population of receptors in the guinea pig ileum are different from those in the mouse vas deferens. These findings also point out the uniqueness of the μ receptor system in the guinea pig ileum which is reflected by the potency differences between naltrexone and naloxone.",

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author = "Takemori, {A. E.} and Portoghese, {P. S.}",

note = "Funding Information: In most of the above studies the antagonistic activity of naltrexone was tested principally against morphine, a prototypical tt-opioid agonist. In this study, we have used the guinea pig ileum and mouse vas deferens preparations and the concept * This work was supported by U.S. Public Health Grants from the National Institute on Drug Abuse. t To whom all correspondence should be addressed: Depart-ment of Pharmacology, 3-260 Millard Hall, University of Minnesota, 435 Delaware Street S.E., Minneapolis, MN 55455, U.S.A.",

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AU - Takemori, A. E.

AU - Portoghese, P. S.

N1 - Funding Information: In most of the above studies the antagonistic activity of naltrexone was tested principally against morphine, a prototypical tt-opioid agonist. In this study, we have used the guinea pig ileum and mouse vas deferens preparations and the concept * This work was supported by U.S. Public Health Grants from the National Institute on Drug Abuse. t To whom all correspondence should be addressed: Depart-ment of Pharmacology, 3-260 Millard Hall, University of Minnesota, 435 Delaware Street S.E., Minneapolis, MN 55455, U.S.A.

PY - 1984/9/3

Y1 - 1984/9/3

N2 - In the guinea pig ileum preparation, naltrexone was 3.5 to 5 times more potent than naloxone in antagonizing morphine but the antagonists were equipotent in antagonizing ethylketazocine. In the mouse vas deferens preparation, naltrexone and naloxone were equipotent in antagonizing both morphine and [D-Ala2-D-Leu5]enkephalin. The data provide evidence that the naltrexone-reversible μ population of receptors in the guinea pig ileum are different from those in the mouse vas deferens. These findings also point out the uniqueness of the μ receptor system in the guinea pig ileum which is reflected by the potency differences between naltrexone and naloxone.

AB - In the guinea pig ileum preparation, naltrexone was 3.5 to 5 times more potent than naloxone in antagonizing morphine but the antagonists were equipotent in antagonizing ethylketazocine. In the mouse vas deferens preparation, naltrexone and naloxone were equipotent in antagonizing both morphine and [D-Ala2-D-Leu5]enkephalin. The data provide evidence that the naltrexone-reversible μ population of receptors in the guinea pig ileum are different from those in the mouse vas deferens. These findings also point out the uniqueness of the μ receptor system in the guinea pig ileum which is reflected by the potency differences between naltrexone and naloxone.

KW - Agonist

KW - Antagonist

KW - Naloxone

KW - Naltrexone

KW - Opioid

KW - Receptor type

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ER -

Comparative antagonism by naltrexone and naloxone of μ, κ, and δ agonists

Abstract

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