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YM 298198 hydrochloride is a 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.
| Molecular Weight | 378.92 |
| Formula | C18H22N4OS.HCl |
| CAS Number | 1216398-09-2 |
| Solubility (25°C) | Water 37.89 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Marciniszyn, et al. J Biol Chem. Mode of inhibition of acid proteases by pepstatin.
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