MGLUR5 ANTAGONIST, MTEP

mGluR5 Antagonist, MTEP
3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine
A brain-permeable (thiazole-pyridine)alkyne compound that acts as a potent, selective and non-competitive mGluR5 (metabotropic glutamate receptor subtype-5) antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM) with in vivo anxiolytic activity in a rodent model (ED50 = 1 mg/kg, ip and 7 mg/kg, po). Devoid of any side effects seen with MPEP and benzodiazepines. Reported to weakly affect the activities of other enzymes and receptors tested (IC50 = 30 µM for MAO-A, > 100 µM for mGlu1R, 2R & 7R, and > 300 µM for NR2BR).
产品信息
Form  Yellowish-white solid
Molar mass  200.3
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥98% by NMR
Solubility  DMSO or MeOH
Chemical formula  C11H8N2S
CAS number  329205-68-7
商店和运输信息
Storage  +2°C to +8°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling