In this study, we attempted to identify the mechanisms of paeoniflorin on a
ntinociceptive effects in mice. Paeoniflorin (48, 96, 240, 480 mug, i.c.v.)
showed dose-related antinociception both on the early and late phases of f
ormalin test in mice. Moreover, paeoniflorin (48 mug, i.c.v.) could potenti
ate the antinociception of morphrine (0.5, 1.0 mg/kg, s.c.) in the formalin
test. However, the antinociceptive effects of paeoniflorin were not potent
iated by L-arginine (600 mg/kg, i.p.) or antagonized by beta -funaltrexamin
e (beta -FNA) (10 mug, i.c.v.), ICI-174,864 (1 mug, i.c.v.) and ryanodine (
10 ng, i.c.v.) on both the early and late phases of formalin test. L-NAME (
75 mg/kg, i.p.) could reverse the effect of paeoniflorin on the late phase
of formalin test. Naloxone (1 mg/kg, i.p.) and nor-binaltorphimine (nor-BNI
) (1 mug, i.c.v.) could block the paeoniflorin-induced antinociception on t
he early phase of formalin test. These results suggested that the central a
ntinociceptive effects of paeoniflorin on formalin test in mice were mediat
ed by the activation of kappa -opioid receptor and not related to the incre
ase of intracellular calcium. (C) 2001 Elsevier Science Ireland Ltd. All ri
ghts reserved.