An NMDA receptor antagonist
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Cerestat

Item No. 30966

Technical Information
Formal Name
N-(3-ethylphenyl)-N-methyl-N′-1-naphthalenyl-guanidine, monohydrochloride
CAS Number
137160-11-3
Synonyms
  • CNS 1102
Molecular Formula
C20H21N3 • HCl
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: 100 mMWater: 50 mM
SMILES
N=C(N(C)C1=CC(CC)=CC=C1)NC2=CC=CC3=C2C=CC=C3.Cl
InChi Code
InChI=1S/C20H21N3.ClH/c1-3-15-8-6-11-17(14-15)23(2)20(21)22-19-13-7-10-16-9-4-5-12-18(16)19;/h4-14H,3H2,1-2H3,(H2,21,22);1H
InChi Key
CKAKVKWRMCAYJD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Cerestat is an NMDA receptor antagonist (IC50 = 36 nM).1 It is selective for the NMDA receptor over sigma receptors (IC50 = 2,540 nM). Cerestat (1 mg/kg) reduces infarct volume and the number of steps and errors in a foot fault test in a rat model of stroke induced by middle cerebral artery occlusion.2 It also reduces cortical and striatal neuronal necrosis in a rat model of temporary focal ischemia when administered at a dose of 1.13 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Reddy, N.L., Hu, L.-Y., Cotter, R.E., et alSynthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: A new, selective noncompetitive NMDA receptor antagonist. J. Med. Chem. 37(2), 260-267 (1994).

    2. Pitsikas, N., Brambilla, A., Besozzi, C., et alEffects of cerestat and NBQX on functional and morphological outcomes in rat focal cerebral ischemia. Pharmacol. Biochem. Behav. 68(3), 443-447 (2000).

    3. Schäbitz, W.R., Li, F., and Fisher, M. The N-methyl-Ⅾ-aspartate antagonist CNS 1102 protects cerebral gray and white matter from ischemic injury following temporary focal ischemia in rats. Stroke 31(7), 1709-1714 (2000).