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

doi:10.1016/0014-2999(94)00716-K

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 journal › Article › peer-review

45 Scopus citations

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 language	English (US)
Pages (from-to)	187-189
Number of pages	3
Journal	European Journal of Pharmacology
Volume	273
Issue number	1-2
DOIs	https://doi.org/10.1016/0014-2999(94)00716-K
State	Published - Jan 24 1995
Externally published	Yes

Keywords

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

ASJC Scopus subject areas

Pharmacology

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10.1016/0014-2999(94)00716-K

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

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.",

keywords = "(CD-1 mouse), Morphine tolerance, NMDA receptor/glycine site antagonist, Tail flick test",

author = "Kabirullah Lutfy and Shen, {Ke Zhong} and Kwon, {Ik Sung} and Cai, {Sui Xiong} and Woodward, {Richard M.} and Keana, {John F.W.} and Eckard Weber",

note = "Funding Information: We are indebted to Silvia Loyola, Minh Nguyen, Kyung Kim, Michelle Cao, Monica Trinh, Peter C. Rim, Peter Doan, Lien Pham, Karyn Wu, Thao Trinh, Olva Kim and Margaret Uhm for technical assistance. This study was supported by NIDA grant DA 06726 and by Acea Pharmaceuticals, Inc.",

year = "1995",

month = jan,

day = "24",

doi = "10.1016/0014-2999(94)00716-K",

language = "English (US)",

volume = "273",

pages = "187--189",

journal = "European Journal of Pharmacology",

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T1 - Blockade of morphine tolerance by ACEA-1328, a novel NMDA receptor/glycine site antagonist

AU - Lutfy, Kabirullah

AU - Shen, Ke Zhong

AU - Kwon, Ik Sung

AU - Cai, Sui Xiong

AU - Woodward, Richard M.

AU - Keana, John F.W.

AU - Weber, Eckard

N1 - Funding Information: We are indebted to Silvia Loyola, Minh Nguyen, Kyung Kim, Michelle Cao, Monica Trinh, Peter C. Rim, Peter Doan, Lien Pham, Karyn Wu, Thao Trinh, Olva Kim and Margaret Uhm for technical assistance. This study was supported by NIDA grant DA 06726 and by Acea Pharmaceuticals, Inc.

PY - 1995/1/24

Y1 - 1995/1/24

N2 - 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.

AB - 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.

KW - (CD-1 mouse)

KW - Morphine tolerance

KW - NMDA receptor/glycine site antagonist

KW - Tail flick test

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

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