CFMTI

Non Antibodies

mGluR1

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

349, 4

A Potent and Selective Antagonist of mGluR1 Receptors

Up to 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

41116134

CFMTI is a selective and potent allosteric antagonist of mGluR1 receptors. It inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a with IC50 values of 2.6 and 2.3 nM, respectively. It is highly selective for mGluR1 over mGluR5 (2000-fold), and does not affect mGluR subtypes and other receptors at 10 µM1.

Yes

CFMTI is a negative allosteric modulator of mGluR1 receptors with IC50 values of 2.6 and 2.3 nM for human and rat mGluR1 expressed in CHO cells, respectively. CFMTI demonstrates high potency and selectivity for the receptor both in vitro and in vivo after oral administration and shows very low potency for other mGluR subtypes1, 2.Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCRs) that play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly expressed on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cells and the formation of the hippocampus3.