FPTQ是mGluR1拮抗剂,在人和老鼠上IC50是6nM和4nM
Cas No. | 864863-72-9 |
Canonical SMILES | FC(N=CC=C1)=C1N2N=NC(C3=CC4=C(C=C3)N=CC=C4)=C2C |
分子式 | C17H12FN5 |
分子量 | 305.31 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. Inhibit [3H] FTIDC target: mGluR1IC 50: 6 nM [1]In vivo: FPTQ exhibited dose-dependent and plasma concentration-dependent receptor occupancy in the cerebellum and striatum. Compound A inhibit (S)-3,5-DHPG-induced face-washing behavior by 46 ± 14% and 97 ± 6.6% (mean ± S.E.M., n = 6) at 10 and 30 mg/kg, respectively.[2] [1]. Fujinaga M et al. Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain. Bioorg Med Chem, 2011 Jan 1, 19(1):102 [2]. Suzuki G et al. Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists. J Pharmacol Sci, 2009 Jul, 110(3):315-25. |