FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC 50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
性状
Solid
IC50 & Target[1][2]
mGluR1a 5.8 nM (IC50) mGlu5 620
体外研究(In Vitro)
FTIDC inhibits L-glutamate-induced increases in intracellular Ca concentrations, with IC50 values of 5.8 nM , 5.8 nM , 3.1 nM , 7.7 nM for human mGluR1a, rat mGluR1a, mouse mGluR1a, human mGluR1b in CHO cells, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FTIDC (i.p. or p.o.; 1-30 mg/kg) reduces the duration of face-washing behavior elicited in a dosedependent manner and the inhibitory effect is statistically significant at 10 and 30 mg/kg with i.p. and 30 mg/kg with p.o.. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Mo
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Suzuki G, et al. Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carbox