| Description |
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1[1].
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| Related Catalog |
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| Target |
mGluR1a:5.8 nM (IC50)
mGluR5:6200 nM (IC50)
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| In Vitro |
FTIDC inhibits L-glutamate-induced increases in intracellular Ca2+ 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[1].
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| 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.[1]. Animal Model: Male CD1 (ICR) mice of 6-weeks-old[1] Dosage: 1, 3, 10, and 30 mg/kg Administration: I.p. or p.o. Result: Reduced the duration of face-washing behavior elicited in a dosedependent manner and was statistically significant at 10 and 30 mg/kg with i.p. and 30 mg/kg with p.o..
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| References |
[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)-carboxamide (FTIDC). J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53.
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