(+)-CP 101,606

CP 101,606 is a noncompetitive antagonist of NMDA receptors containing the NR2B subunit (Kd = 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 (Cay-92350) and phorbol-12-myristate-13-acetate (PMA, Cay-10008014, ED50s = 7.5 and 5.7 mg/kg, respectively). CP 101,606 reverses catalepsy in rats induced by haloperidol (Cay-12014) 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 (Cay-16149) temporarily improves parkinsonian symptoms in an MPTP model of Parkinson's disease in rhesus monkeys.Formal Name: 4-hydroxy-alphaS-(4-hydroxyphenyl)-betaS-methyl-4-phenyl-1-piperidineethanol. CAS Number: 134234-12-1. Synonyms: CP 98,113. Molecular Formula: C20H25NO3. Formula Weight: 327.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 2 mg/ml, Ethanol: 2 mg/ml. lambdamax: 227, 279 nm. SMILES: OC1=CC=C([C@H](O)[C@H](C)N2CCC(C3=CC=CC=C3)(O)CC2)C=C1. InChi Code: InChI=1S/C20H25NO3/c1-15(19(23)16-7-9-18(22)10-8-16)21-13-11-20(24,12-14-21)17-5-3-2-4-6-17/h2-10,15,19,22-24H,11-14H2,1H3/t15-,19+/m0/s1. InChi Key: QEMSVZNTSXPFJA-HNAYVOBHSA-N.