Flunarizine analgesia is mediated by μ-opioid receptors

Ronit Weizman; Irena A. Pankova; Shaul Schreiber; Chaim G. Pick

doi:10.1016/S0031-9384(97)00344-2

Flunarizine analgesia is mediated by μ-opioid receptors

Ronit Weizman, Irena A. Pankova, Shaul Schreiber, Chaim G. Pick^*

^*Corresponding author for this work

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

Abstract

We evaluated the opioid antinociceptive mechanism of the calcium channel blocker flunarizine. Flunarizine produced a dose-dependent analgesia in the hot plate test which was antagonized by general (naloxone) and μ [beta-fualtrexamine (β-FNA)]-opioid antagonists, indicating a role for μ receptors in flunarizine analgesia. Naltrindole (δ₁ antagonist) did not affect flunarizine analgesia. A fixed subthreshold dose of flunarizine augmented μ (morphine) analgesia and blocked δ₁, [enkephalin, [D-Pen^2,5] (DPDPE)] analgesia. Apparently, flunarizine has μ agonistic activity and δ₁, antagonist or mixed agonistic-antagonistic activity.

Original language	English
Pages (from-to)	1193-1195
Number of pages	3
Journal	Physiology and Behavior
Volume	62
Issue number	5
DOIs	https://doi.org/10.1016/S0031-9384(97)00344-2
State	Published - Nov 1997

Keywords

Analgesia
Flunarizine
Opioid receptor subtypes

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10.1016/S0031-9384(97)00344-2

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title = "Flunarizine analgesia is mediated by μ-opioid receptors",

abstract = "We evaluated the opioid antinociceptive mechanism of the calcium channel blocker flunarizine. Flunarizine produced a dose-dependent analgesia in the hot plate test which was antagonized by general (naloxone) and μ [beta-fualtrexamine (β-FNA)]-opioid antagonists, indicating a role for μ receptors in flunarizine analgesia. Naltrindole (δ1 antagonist) did not affect flunarizine analgesia. A fixed subthreshold dose of flunarizine augmented μ (morphine) analgesia and blocked δ1, [enkephalin, [D-Pen2,5] (DPDPE)] analgesia. Apparently, flunarizine has μ agonistic activity and δ1, antagonist or mixed agonistic-antagonistic activity.",

keywords = "Analgesia, Flunarizine, Opioid receptor subtypes",

author = "Ronit Weizman and Pankova, {Irena A.} and Shaul Schreiber and Pick, {Chaim G.}",

note = "Funding Information: This work was supported in part by the Tel Aviv University Foundation for Basic Research and by a research grant from The Adams Super-Center for Brain Studies at Tel Aviv University. ",

year = "1997",

month = nov,

doi = "10.1016/S0031-9384(97)00344-2",

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AU - Weizman, Ronit

AU - Pankova, Irena A.

AU - Schreiber, Shaul

AU - Pick, Chaim G.

N1 - Funding Information: This work was supported in part by the Tel Aviv University Foundation for Basic Research and by a research grant from The Adams Super-Center for Brain Studies at Tel Aviv University.

PY - 1997/11

Y1 - 1997/11

N2 - We evaluated the opioid antinociceptive mechanism of the calcium channel blocker flunarizine. Flunarizine produced a dose-dependent analgesia in the hot plate test which was antagonized by general (naloxone) and μ [beta-fualtrexamine (β-FNA)]-opioid antagonists, indicating a role for μ receptors in flunarizine analgesia. Naltrindole (δ1 antagonist) did not affect flunarizine analgesia. A fixed subthreshold dose of flunarizine augmented μ (morphine) analgesia and blocked δ1, [enkephalin, [D-Pen2,5] (DPDPE)] analgesia. Apparently, flunarizine has μ agonistic activity and δ1, antagonist or mixed agonistic-antagonistic activity.

AB - We evaluated the opioid antinociceptive mechanism of the calcium channel blocker flunarizine. Flunarizine produced a dose-dependent analgesia in the hot plate test which was antagonized by general (naloxone) and μ [beta-fualtrexamine (β-FNA)]-opioid antagonists, indicating a role for μ receptors in flunarizine analgesia. Naltrindole (δ1 antagonist) did not affect flunarizine analgesia. A fixed subthreshold dose of flunarizine augmented μ (morphine) analgesia and blocked δ1, [enkephalin, [D-Pen2,5] (DPDPE)] analgesia. Apparently, flunarizine has μ agonistic activity and δ1, antagonist or mixed agonistic-antagonistic activity.

KW - Analgesia

KW - Flunarizine

KW - Opioid receptor subtypes

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EP - 1195

JO - Physiology and Behavior

JF - Physiology and Behavior

IS - 5

ER -

Flunarizine analgesia is mediated by μ-opioid receptors

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Keywords

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