An antagonist of NR2B subunit-containing NMDA receptors
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(+)-CP 101,606

Item No. 23884

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-hydroxy-αS-(4-hydroxyphenyl)-βS-methyl-4-phenyl-1-piperidineethanol
CAS Number
134234-12-1
Synonyms
  • CP 98,113
Molecular Formula
C20H25NO3
Formula Weight
327.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 2 mg/mlEthanol: 2 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $80

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    10 mg

    $103

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    25 mg

    $235

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    Product Description

    CP 101,606 is a noncompetitive antagonist of NMDA receptors containing the NR2B subunit (Kd = 4.2 nM).1 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.2 It also inhibits licking behavior in rats induced by capsaicin (Item No. 92350) and phorbol-12-myristate-13-acetate (PMA; Item No. 10008014; ED50s = 7.5 and 5.7 mg/kg, respectively). CP 101,606 reverses catalepsy in rats induced by haloperidol (Item No. 12014) with an ED50 value of 0.4 mg/kg.3 CP 101,606 (1 mg/kg, s.c.) alone or in combination with L-DOPA methyl ester (Item No. 16149) temporarily improves parkinsonian symptoms in an MPTP model of Parkinson's disease in rhesus monkeys.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chazot, P.L., Lawrence, S., and Thompson, C.L. Studies on the subtype selectivity of CP-101,606: Evidence for two classes of NR2B-selective NMDA receptor antagonists. Neuropharmacology 42(3), 319-324 (2002).

    2. Taniguchi, K., Shinjo, K., Mizutani, M., et al. Antinociceptive activity of CP-101,606, an NMDA receptor NR2B subunit antagonist. Br. J. Pharmacol. 122(5), 809-812 (1997).

    3. Steece-Collier, K., Chambers, L.K., Jaw-Tsai, S.S., et al. Antiparkinsonian actions of CP-101,606, an antagonist of NR2B subunit-containing N-methyl-d-aspartate receptors. Exp. Neurol. 163(1), 239-243 (2000).