A non-competitive antagonist of mGluR1
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YM-298198 (hydrochloride)

Item No. 22925

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]benzimidazole-2-carboxamide, monohydrochloride
CAS Number
1216398-09-2
Molecular Formula
C18H22N4OS • HCl
Formula Weight
378.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 25 mg/mlDMSO:PBS (pH 7.2)(1:8): 0.11 m/gml
λmax
220, 252 nm
SMILES
NC1=CC=C2C(N(C(C)=C(C(N(C)C3CCCCC3)=O)S4)C4=N2)=C1.Cl
InChi Code
InChI=1S/C18H22N4OS.ClH/c1-11-16(17(23)21(2)13-6-4-3-5-7-13)24-18-20-14-9-8-12(19)10-15(14)22(11)18;/h8-10,13H,3-7,19H2,1-2H3;1H
InChi Key
WYTJVUVCSUWZTH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    25 mg

    $534

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    Product Description

    YM-298198 is a non-competitive antagonist of the metabotropic glutamate receptor type I (mGluR1; Ki = 19 nM).1 It is selective for mGluR1 over mGluR2-7 (IC50s = 0.016 and >10 μM, respectively). YM-298198 binds to rat cerebellum membranes (Ki = 20 nM). In vivo, YM-298198 (10 and 30 mg/kg, p.o.) increases nociceptive response latency in a mouse model of hyperalgesia induced by streptozotocin (Item No. 13104) without affecting motor coordination in a rotarod test. YM-298198 also reduces reinstatement of drug-seeking behavior induced by cocaine priming in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kohara, A., Toya, T., Tamura, S., et al. Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1. J. Pharmacol. Exp. Ther. 315(1), 163-169 (2005).

    2. Schmidt, H.D., Kimmey, B.A., Arreola, A.C., et al. Group I metabotropic glutamate receptor-mediated activation of PKC gamma in the nucleus accumbens core promotes the reinstatement of cocaine seeking. Addict. Biol. 20(2), 285-296 (2015).