Pharmacological profiles of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) on the mouse vas deferens preparation

Susan J. Ward; Philip S Portoghese; A. E. Takemori

doi:10.1016/0014-2999(82)90083-8

Pharmacological profiles of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) on the mouse vas deferens preparation

Susan J. Ward, Philip S Portoghese, A. E. Takemori

Medicinal Chemistry

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

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Abstract

The profiles of action of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) have been assessed in the mouse vas deferens preparation. β-FNA, but not β-CNA, demonstrated a reversible agonist action that appeared to be mediated via κ-receptor interaction. β-CNA produced an irreversible antagonism of μ-, κ- and δ-mediated agonist actions, whereas β-FNA irreversibly antagonized μ-mediated agonist effects only. This selective action of β-FNA could also be seen following administration in vivo. β-CNA and particularly β-FNA should prove valuable in the elucidation of multiple opioid receptors.

Original language	English (US)
Pages (from-to)	377-384
Number of pages	8
Journal	European Journal of Pharmacology
Volume	80
Issue number	4
DOIs	https://doi.org/10.1016/0014-2999(82)90083-8
State	Published - Jun 4 1982

Bibliographical note

Funding Information:
i This investigation was supported by U.S. Public Health Grants DA 00289 and 01533 from the National Institute on Drug Abuse.

Keywords

Mouse vas deferens
Multiple receptors
Selective antagonism
β-CNA
β-FNA

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10.1016/0014-2999(82)90083-8

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title = "Pharmacological profiles of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) on the mouse vas deferens preparation",

abstract = "The profiles of action of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) have been assessed in the mouse vas deferens preparation. β-FNA, but not β-CNA, demonstrated a reversible agonist action that appeared to be mediated via κ-receptor interaction. β-CNA produced an irreversible antagonism of μ-, κ- and δ-mediated agonist actions, whereas β-FNA irreversibly antagonized μ-mediated agonist effects only. This selective action of β-FNA could also be seen following administration in vivo. β-CNA and particularly β-FNA should prove valuable in the elucidation of multiple opioid receptors.",

keywords = "Mouse vas deferens, Multiple receptors, Selective antagonism, β-CNA, β-FNA",

author = "Ward, {Susan J.} and Portoghese, {Philip S} and Takemori, {A. E.}",

note = "Funding Information: i This investigation was supported by U.S. Public Health Grants DA 00289 and 01533 from the National Institute on Drug Abuse.",

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doi = "10.1016/0014-2999(82)90083-8",

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T1 - Pharmacological profiles of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) on the mouse vas deferens preparation

AU - Ward, Susan J.

AU - Portoghese, Philip S

AU - Takemori, A. E.

N1 - Funding Information: i This investigation was supported by U.S. Public Health Grants DA 00289 and 01533 from the National Institute on Drug Abuse.

PY - 1982/6/4

Y1 - 1982/6/4

N2 - The profiles of action of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) have been assessed in the mouse vas deferens preparation. β-FNA, but not β-CNA, demonstrated a reversible agonist action that appeared to be mediated via κ-receptor interaction. β-CNA produced an irreversible antagonism of μ-, κ- and δ-mediated agonist actions, whereas β-FNA irreversibly antagonized μ-mediated agonist effects only. This selective action of β-FNA could also be seen following administration in vivo. β-CNA and particularly β-FNA should prove valuable in the elucidation of multiple opioid receptors.

AB - The profiles of action of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) have been assessed in the mouse vas deferens preparation. β-FNA, but not β-CNA, demonstrated a reversible agonist action that appeared to be mediated via κ-receptor interaction. β-CNA produced an irreversible antagonism of μ-, κ- and δ-mediated agonist actions, whereas β-FNA irreversibly antagonized μ-mediated agonist effects only. This selective action of β-FNA could also be seen following administration in vivo. β-CNA and particularly β-FNA should prove valuable in the elucidation of multiple opioid receptors.

KW - Mouse vas deferens

KW - Multiple receptors

KW - Selective antagonism

KW - β-CNA

KW - β-FNA

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JF - European Journal of Pharmacology

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Pharmacological profiles of β-funaltrexamine (β-FNA) and β-chlornaltrexamine (β-CNA) on the mouse vas deferens preparation

Abstract

Bibliographical note

Keywords

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