Lack of antinociceptive efficacy of intracerebroventricular [D-Ala2,Glu4]deltorphin, but not [D-Pen2,D-Pen5]enkephalin, in the μ-opioid receptor deficient CXBX mouse

Robert B. Raffa, Rebecca P. Martinez, Frank Porreca

Research output: Contribution to journalArticle

23 Citations (Scopus)

Abstract

The antinociceptive efficacy of [D-Pen2,D-Pen5]enkephalin (DPDPE) (δ1agonist) and [D-Ala2,Glu4]deltorphin (δ2agonist) was evaluated following intracerebroventricular (i.c.v.) or intrathecal (i.t.) administration in CD-1 and CXBK strains of mice using the radiant heat tail-flick test. Following i.c.v. administration, [D-Ala2,Glu4]deltorphin was effective in CD-1, but not CXBK, mice; DPDPE was approximately equiactive in both strains. While i.c.v. [D-Ala2,Glu4]deltorphin did not produce antinociception in the CXBK mouse, it effectively antagonized the antinociceptive actions if i.c.v. DPDPE. [D-Ala2,Glu4]deltorphin was effective following i.t. administration in both strains. These data suggest possible differences in the supraspinal populations of opioid δ receptor subtypes in the CXBK strain. On the basis of previously established selectivity of these agonists, the CXBK mouse may have a predominate population of supraspinal opioid δ1, rather than δ2, receptors.

Original languageEnglish (US)
Pages (from-to)453-456
Number of pages4
JournalEuropean Journal of Pharmacology
Volume216
Issue number3
DOIs
StatePublished - Jun 17 1992
Externally publishedYes

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D-Penicillamine (2,5)-Enkephalin
Opioid Receptors
Opioid Analgesics
Population
Tail
Hot Temperature
deltorphin

Keywords

  • Antinociception
  • CD-1 mice
  • CXBK mice
  • DPDPE ([D-Pen,D-Pen]enkephalin)
  • [D-Ala,Glu]deltorphin
  • δ-Opioid receptor subtypes

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

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title = "Lack of antinociceptive efficacy of intracerebroventricular [D-Ala2,Glu4]deltorphin, but not [D-Pen2,D-Pen5]enkephalin, in the μ-opioid receptor deficient CXBX mouse",
abstract = "The antinociceptive efficacy of [D-Pen2,D-Pen5]enkephalin (DPDPE) (δ1agonist) and [D-Ala2,Glu4]deltorphin (δ2agonist) was evaluated following intracerebroventricular (i.c.v.) or intrathecal (i.t.) administration in CD-1 and CXBK strains of mice using the radiant heat tail-flick test. Following i.c.v. administration, [D-Ala2,Glu4]deltorphin was effective in CD-1, but not CXBK, mice; DPDPE was approximately equiactive in both strains. While i.c.v. [D-Ala2,Glu4]deltorphin did not produce antinociception in the CXBK mouse, it effectively antagonized the antinociceptive actions if i.c.v. DPDPE. [D-Ala2,Glu4]deltorphin was effective following i.t. administration in both strains. These data suggest possible differences in the supraspinal populations of opioid δ receptor subtypes in the CXBK strain. On the basis of previously established selectivity of these agonists, the CXBK mouse may have a predominate population of supraspinal opioid δ1, rather than δ2, receptors.",
keywords = "Antinociception, CD-1 mice, CXBK mice, DPDPE ([D-Pen,D-Pen]enkephalin), [D-Ala,Glu]deltorphin, δ-Opioid receptor subtypes",
author = "Raffa, {Robert B.} and Martinez, {Rebecca P.} and Frank Porreca",
year = "1992",
month = "6",
day = "17",
doi = "10.1016/0014-2999(92)90446-B",
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T1 - Lack of antinociceptive efficacy of intracerebroventricular [D-Ala2,Glu4]deltorphin, but not [D-Pen2,D-Pen5]enkephalin, in the μ-opioid receptor deficient CXBX mouse

AU - Raffa, Robert B.

AU - Martinez, Rebecca P.

AU - Porreca, Frank

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N2 - The antinociceptive efficacy of [D-Pen2,D-Pen5]enkephalin (DPDPE) (δ1agonist) and [D-Ala2,Glu4]deltorphin (δ2agonist) was evaluated following intracerebroventricular (i.c.v.) or intrathecal (i.t.) administration in CD-1 and CXBK strains of mice using the radiant heat tail-flick test. Following i.c.v. administration, [D-Ala2,Glu4]deltorphin was effective in CD-1, but not CXBK, mice; DPDPE was approximately equiactive in both strains. While i.c.v. [D-Ala2,Glu4]deltorphin did not produce antinociception in the CXBK mouse, it effectively antagonized the antinociceptive actions if i.c.v. DPDPE. [D-Ala2,Glu4]deltorphin was effective following i.t. administration in both strains. These data suggest possible differences in the supraspinal populations of opioid δ receptor subtypes in the CXBK strain. On the basis of previously established selectivity of these agonists, the CXBK mouse may have a predominate population of supraspinal opioid δ1, rather than δ2, receptors.

AB - The antinociceptive efficacy of [D-Pen2,D-Pen5]enkephalin (DPDPE) (δ1agonist) and [D-Ala2,Glu4]deltorphin (δ2agonist) was evaluated following intracerebroventricular (i.c.v.) or intrathecal (i.t.) administration in CD-1 and CXBK strains of mice using the radiant heat tail-flick test. Following i.c.v. administration, [D-Ala2,Glu4]deltorphin was effective in CD-1, but not CXBK, mice; DPDPE was approximately equiactive in both strains. While i.c.v. [D-Ala2,Glu4]deltorphin did not produce antinociception in the CXBK mouse, it effectively antagonized the antinociceptive actions if i.c.v. DPDPE. [D-Ala2,Glu4]deltorphin was effective following i.t. administration in both strains. These data suggest possible differences in the supraspinal populations of opioid δ receptor subtypes in the CXBK strain. On the basis of previously established selectivity of these agonists, the CXBK mouse may have a predominate population of supraspinal opioid δ1, rather than δ2, receptors.

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