YM 298198 hydrochloride

Name: YM 298198 hydrochloride
Brand: Tocris Bioscience
SKU: 2448

Tocris Bioscience, part of Bio-Techne | Catalog # 2448

Citations (45)

COA / SDS

Highly potent, selective non-competitive mGlu1 antagonist

Discontinued Product

2448 has been discontinued. View all Group I mGluR Antagonists products.

Key Product Details

Description:	Highly potent, selective non-competitive mGlu₁ antagonist
Chemical Name:	6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	378.92

View Full Technical Details for YM 298198 hydrochloride

Technical Data
Citations

Biological Activity for YM 298198 hydrochloride

YM 298198 hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu₁ receptors (K_i = 19 nM); inactive at other mGlu receptor subtypes (mGlu_2-7), ionotropic receptors and glutamate transporters (IC₅₀ > 10 μM). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC₅₀ values are 16 nM and 6.3 μM respectively), and is orally active in vivo, demonstrating an antinociceptive effect in hyperalgesic mice.

Desmethyl Derivative also available.

Licensing Information

Sold with the permission of Astellas Pharma Inc.

Technical Data for YM 298198 hydrochloride

M. Wt	378.92
Formula	C₁₈H₂₂N₄OS.HCl
Storage	Desiccate at +4°C
Purity	≥99% (HPLC)
CAS Number	1216398-09-2
PubChem ID	45073464
InChi Key	WYTJVUVCSUWZTH-UHFFFAOYSA-N
Smiles	Cl.CN(C1CCCCC1)C(=O)C1=C(C)N2C(S1)=NC1=CC=C(N)C=C21

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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References for YM 298198 hydrochloride

References are publications that support the biological activity of the product.

Emery The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation. J.Biol.Chem. 2010 PMID: 20566651
Kohara Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective and noncompetitive antagonist of metabo J.Pharmacol.Exp.Ther. 2005 PMID: 15976016