Abstract |
(+)-(1-Hydroxy-3-aminopyrrolidine-2-one) ((+)- HA 966), a partial agonist at the glycine site coupled to N-methyl-D-aspartic acid ( NMDA) receptors, abolished the late phase of licking induced by injection of formalin into the hind-paw of mice; inhibitory dose50 (ID50) = 1.6 mg/kg, s.c. In contrast, it was weakly active against the first phase; ID50 = 33.3 mg/kg, s.c. Further, (+)- HA 966 was inactive in the rotarod test of ataxia. These data support a role of NMDA receptors in the transmission of prolonged noxious stimulation and suggest that partial glycine receptor agonists may exert antinociceptive properties against persistent pain.
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Authors | M J Millan, L Seguin |
Journal | European journal of pharmacology
(Eur J Pharmacol)
Vol. 238
Issue 2-3
Pg. 445-7
(Jul 20 1993)
ISSN: 0014-2999 [Print] Netherlands |
PMID | 8405116
(Publication Type: Journal Article)
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Chemical References |
- Pyrrolidinones
- Receptors, N-Methyl-D-Aspartate
- Formaldehyde
- 1-hydroxy-3-amino-2-pyrrolidone
- Glycine
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Topics |
- Animals
- Formaldehyde
(toxicity)
- Glycine
(metabolism)
- Hindlimb
- Male
- Mice
- Pain
(chemically induced, drug therapy)
- Pyrrolidinones
(pharmacology, therapeutic use)
- Receptors, N-Methyl-D-Aspartate
(drug effects, metabolism)
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