NMDAR Polvamine-like Antagonists - Based on localization, biochemical and pharmacological data, it has been hypothesized that NR2B subunits preferentially mediate pain transmission. Traxoprodil (CP-101606,4) has a binding affinity (Kd) of 10 nM and dose-dependently reversed L5/L6 sciatic nerve ligation (SNL)-induced mechanical hypersensitivity (3-10 mg/kg; i.p.). A 10-fold higher dose did not produce disturbances in motor coordination (20,21). More recently synthesized benzamide derivatives have greater than 20,000-fold selectivity for recombinant NR1/NR2B receptors than for NR1/NR2A receptors (22). Related piperazine 5 had good oral bioavailability as indicated by ED5o values of 5.5 to 16 mg/kg for reversing carrageenan-induced hypersensitivity (23). These findings suggest that NR2B selective antagonists might have clinical utility in treating neuropathic pain with reduced adverse effects compared to non-selective antagonists.
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