Cayman (+)-CP 101,606

CP 101,606 is a noncompetitive antagonist of NMDA receptors containing the NR2B subunit (K_d = 4.2 nM). CP 101,606 is highly selective for NR1/NR2B-containing NMDA receptors over NR1, NR2A, and NR2B subunits alone and NR1/NR2A receptors in HEK293 cell homogenates. In vivo, CP 101,606 (30 mg/kg, s.c.) inhibits mechanical hyperalgesia following carrageenan challenge in rats. It also inhibits licking behavior in rats induced by capsaicin (Item No. ) and phorbol-12-myristate-13-acetate (PMA; Item No. ; ED₅₀s = 7.5 and 5.7 mg/kg, respectively). CP 101,606 reverses catalepsy in rats induced by haloperidol (Item No. ) with an ED₅₀ value of 0.4 mg/kg. CP 101,606 (1 mg/kg, s.c.) alone or in combination with L-DOPA methyl ester (Item No. ) temporarily improves parkinsonian symptoms in an MPTP model of Parkinsons disease in rhesus monkeys.

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