(+)-HA 966, a partial agonist at the glycine site coupled to NMDA receptors, blocks formalin-induced pain in mice.

(+)-(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.
AuthorsM J Millan, L Seguin
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 238 Issue 2-3 Pg. 445-7 (Jul 20 1993) ISSN: 0014-2999 [Print] NETHERLANDS
PMID8405116 (Publication Type: Journal Article)
Chemical References
  • Pyrrolidinones
  • Receptors, N-Methyl-D-Aspartate
  • 1-hydroxy-3-amino-2-pyrrolidone
  • Formaldehyde
  • Glycine
  • 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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