The glycine B receptor partial agonist, (+)-HA966, enhances induction of antinociception by RP 67580 and CP-99,994

Eur J Pharmacol. 1994 Feb 21;253(1-2):R1-3. doi: 10.1016/0014-2999(94)90777-3.

Abstract

The tachykinin receptor antagonists (3aR,7aR)-7,7-diphenyl-2(1-imino-2-(2-methoxyphenyl/ethyl)++ +perhydroisoindole) (RP 67580) and (+)-(2S-3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine (CP-99,994), which act selectively at neurokinin (NK)1 receptors, inhibited the early phase of formalin-induced pain in mice. Although (+)-(1-hydroxy-3-aminopyrrolidine-2-one) ((+)-HA966), a partial agonist at glycine B receptors, was inactive alone, it potentiated the actions of RP 67580 (but not its inactive stereoisomer, RP68651) and CP-99,994. In its presence, the dose-response curve for RP 67580 was dose-dependently shifted to the left. In contrast, (+)-HA966 did not modify the induction of ataxia by RP 67580 and CP-99,994. These data suggest that co-administration of partial agonists at glycine B receptors may improve the antinociceptive potency and 'therapeutic window' of tachykinin NK1 receptor antagonists.

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Behavior, Animal / drug effects
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Glycine / metabolism
  • Indoles / pharmacology*
  • Isoindoles
  • Male
  • Mice
  • Piperidines / pharmacology*
  • Pyrrolidinones / pharmacology*
  • Receptors, Glycine / drug effects
  • Receptors, Tachykinin / antagonists & inhibitors

Substances

  • Analgesics
  • Indoles
  • Isoindoles
  • Piperidines
  • Pyrrolidinones
  • Receptors, Glycine
  • Receptors, Tachykinin
  • 7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one
  • 3-(2-methoxybenzylamino)-2-phenylpiperidine
  • 1-hydroxy-3-amino-2-pyrrolidone
  • Glycine