Blockade of morphine tolerance by ACEA-1328, a novel NMDA receptor/glycine site antagonist

Kabirullah Lutfy, Ke-Zhong Shen, Ik Sung Kwon, Sui Xiong Cai, Richard M. Woodward, John F W Keana, Eckard Weber

Research output: Contribution to journalArticle

45 Citations (Scopus)

Abstract

Recent studies indicate that competitive and non-competitive NMDA receptor antagonists can block the development of morphine tolerance. Since glycine is considered to be a co-agonist for activation of NMDA receptors we examined the effect of a novel bioavailable NMDA receptor/glycine site antagonist, 5-nitro-6,7-dimethyl-1,4-dihydro-2,3-quinoxalinedione (ACEA-1328), on the development of morphine tolerance. Administration of ACEA-1328 (20 mg/kg) completely blocked tolerance to morphine-induced antinociception in the tail flick test in CD-1 mice, without affecting the basal nociceptive response or potentiating morphine-induced antinociceptive effects. These data suggest that inhibition of NMDA receptor activity via blockade of the glycine co-agonist site is potentially viable as a therapeutic approach for preventing development of morphine tolerance.

Original languageEnglish (US)
Pages (from-to)187-189
Number of pages3
JournalEuropean Journal of Pharmacology
Volume273
Issue number1-2
DOIs
StatePublished - Jan 24 1995
Externally publishedYes

Fingerprint

N-Methyl-D-Aspartate Receptors
Glycine
Morphine
Tail
ACEA 1328
Therapeutics

Keywords

  • (CD-1 mouse)
  • Morphine tolerance
  • NMDA receptor/glycine site antagonist
  • Tail flick test

ASJC Scopus subject areas

  • Pharmacology
  • Cellular and Molecular Neuroscience

Cite this

Blockade of morphine tolerance by ACEA-1328, a novel NMDA receptor/glycine site antagonist. / Lutfy, Kabirullah; Shen, Ke-Zhong; Kwon, Ik Sung; Cai, Sui Xiong; Woodward, Richard M.; Keana, John F W; Weber, Eckard.

In: European Journal of Pharmacology, Vol. 273, No. 1-2, 24.01.1995, p. 187-189.

Research output: Contribution to journalArticle

Lutfy, Kabirullah ; Shen, Ke-Zhong ; Kwon, Ik Sung ; Cai, Sui Xiong ; Woodward, Richard M. ; Keana, John F W ; Weber, Eckard. / Blockade of morphine tolerance by ACEA-1328, a novel NMDA receptor/glycine site antagonist. In: European Journal of Pharmacology. 1995 ; Vol. 273, No. 1-2. pp. 187-189.
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