FPTQ

• CAT Number: I005191
• CAS Number: 864863-72-9
• Molecular Formula: C17H12FN5
• Molecular Weight: 305.316
• Purity: ≥95%
• Target: mGluR1
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 6 nM
• IUPAC Name: 6-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]quinoline
• InChI: InChI=1S/C17H12FN5/c1-11-16(13-6-7-14-12(10-13)4-2-8-19-14)21-22-23(11)15-5-3-9-20-17(15)18/h2-10H,1H3
• InChIKey: RTUBNVSZHGWRCV-UHFFFAOYSA-N
• SMILES: CC1=C(N=NN1C2=C(N=CC=C2)F)C3=CC4=C(C=C3)N=CC=C4

FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. 
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]

Reference

[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):102-10.
[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.