Journal
PHARMACOLOGY
Volume 81, Issue 2, Pages 144-150Publisher
KARGER
DOI: 10.1159/000110737
Keywords
subunit alpha(2)delta; [H-3]-gabapentin; PD-217014; trinitrobenzene sulfonic acid; visceral hypersensitivity; voltage-gated calcium channel
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PD-217014, a new GABA analog (1 alpha,3 alpha,5 alpha-3-aminomethyl-bicyclo[3.2.0] heptane-3-acetic acid), inhibited [H-3]-gabapentin binding to alpha(2)delta subunit of voltage-gated calcium channels in a concentration-dependent manner (K-i = 18 nmol/l). Oral treatment with PD-217014 significantly inhibited the visceral hypersensitivity induced by an intra-colonic injection of trinitrobenzene sulfonic acid in rats. The anti-hyperalgesic effect of PD-217014 increased in a dose-dependent manner, and reached a plateau level at 60 mg/kg p.o. The visceral analgesia produced by PD-217014 at 30 and 60 mg/kg p.o. correlated with blood concentrations within 4 h after dosing, and maximal efficacy was obtained 2 h after dosing when the maximal blood concentration was achieved at either dose. These results indicate that PD-217014 is a potent alpha(2)delta ligand and possesses visceral analgesic activity. Copyright (C) 2008 S. Karger AG, Basel.
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