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Category:
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7TM Receptors Glutamate (Metabotropic) ReceptorsGroup I mGlu ReceptorsAntagonists
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Cat.No.
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Product Name
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2448 |
YM 298198 hydrochloride
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Price and Availability
Click here for full price details of
YM 298198
Other Information:
Sold with the permission of Astellas Pharma Inc.
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Chemical Name:
6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimi
dazole-2-carboxamide hydrochloride |
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Biological Activity:
Non-competitive antagonist with high affinity
and selectivity for mGlu1 receptors (Ki = 19 nM);
inactive at other mGlu receptor subtypes (mGlu2-7), 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.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Kohara et al (2005) 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
metabotropic glutamate receptor type 1. J.Pharmacol.Exp.Ther. 315 163.
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or by Research Area
Keywords: YM 298198, Glutamate (Metabotropic) Receptors, Highly Potent, Selective Non-competitive MGlu1 Antagonist, YM298198, Tocris Bioscience
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