Non-competitive antagonist with high affinity and selectivity for mGlu1
= 19 nM); inactive at other mGlu receptor subtypes (mGlu2-7
), ionotropic receptors and glutamate transporters (IC50
> 10 μ
M). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC50
values are 16 nM and 6.3 μ
M respectively), and is orally active in vivo
, demonstrating an antinociceptive effect in hyperalgesic mice. Desmethyl derivative
(Cat. No. 2447) also available.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Sold with the permission of Astellas Pharma Inc.
Other Product-Specific Information:
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