An antagonist of NR2B subunit-containing NMDA receptors
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BZAD-01

Item No. 38788

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(trifluoromethoxy)-N-[[2-(trifluoromethyl)phenyl]methyl]-benzenecarboximidamide
CAS Number
305339-41-7
Molecular Formula
C16H12F6N2O
Formula Weight
362.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Soluble
SMILES
FC(F)(OC1=CC=C(C(NCC2=C(C(F)(F)F)C=CC=C2)=N)C=C1)F
InChi Code
InChI=1S/C16H12F6N2O/c17-15(18,19)13-4-2-1-3-11(13)9-24-14(23)10-5-7-12(8-6-10)25-16(20,21)22/h1-8H,9H2,(H2,23,24)
InChi Key
YGOCAMFQDLFNQK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $28

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    5 mg

    $97

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    10 mg

    $152

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    25 mg

    $310

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    Product Description

    BZAD-01 is an antagonist of NR2B subunit-containing NMDA receptors (Ki = 72 nM).1 It is selective for NR2B subunit-containing NMDA receptors over those containing NR2A subunits in a calcium mobilization assay (IC50s = 47 and >10,000 nM, respectively). Oral administration of BZAD-01 reduces hyperalgesia induced by carrageenan in rats (ED50 = 5.5 mg/kg). BZAD-01 (10 mg/kg) reduces dopaminergic neuron loss in the rat substantia nigra pars compacta and improves measures of ipsilateral curling, ipsilateral head positioning, and beam walking in a rat model of Parkinson’s disease induced by the catecholaminergic neurotoxin 6-OHDA (Item No. 25330).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Claiborne, C.F., McCauley, J.A., Libby, B.E., et al. Orally efficacious NR2B-selective NMDA receptor antagonists. Bioorg. Med. Chem. Lett. 13(4), 697-700 (2003).

    2. Leaver, K.R., Allbutt, H.N., Creber, N.J., et al. Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson’s disease. Clin. Exp. Pharmacol. Physiol. 35(11), 1388-1394 (2008).