生物学描述Brain penetrant, potent, selective and non-competitive mGlu5 receptor antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM). In vivo anxiolytic, devoid of side effects seen with MPEP and benzodiazepines. Also available in Kit: mGlu antagonists (ab120322).
Also available in simple stock solutions (ab144485) - add 1 ml of water to get an exact, ready-to-use concentration.
存放说明Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
溶解度概述Soluble in water to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Varty GB et al. The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles. Psychopharmacology (Berl)179:207-17 (2005).
Read more (PubMed: 15682298) »
Cosford ND et al. 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J Med Chem46:204-6 (2003).
Read more (PubMed: 12519057) »
Anderson JJ et al. In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). Eur J Pharmacol473:35-40 (2003).
Read more (PubMed: 12877935) »