A-841720

A-841720 is a noncompetitive antagonist of the group 1 metabotropic glutamate receptor mGluR1 with an IC50 value of 10.7 nM for inhibition of L-glutamate-induced calcium release in 1321 N1 cells. It is selective for mGluR1 over mGluR5 (IC50 = 343 nM) as well as mGluR2, mGluR4, and mGluR7, where it does not inhibit agonist-induced calcium release in HEK293 cells. It is also selective for mGluR1 over a panel of other G-coupled protein receptors as well as ligand- and voltage-gated ion channels at a concentration of 10 µM. A-841720 dose-dependently inhibits complete Freund's adjuvant-induced inflammatory pain (ED50 = 23 µmol/kg) and sciatic nerve injury-induced mechanical allodynia (ED50 = 28 µmol/kg) in rats. It also enhances cocaine seeking in mice after a prolonged abstinence following a single conditioning session when administered at a dose of 10 mg/kg per day.Formal Name: 9-(dimethylamino)-3-(hexahydro-1H-azepin-1-yl)-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one. CAS Number: 869802-58-4. Molecular Formula: C17H21N5OS. Formula Weight: 343.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 3 mg/ml. lambdamax: 226, 246, 256, 363 nm. SMILES: O=C1N(N2CCCCCC2)C=NC3=C1SC4=C3C(N(C)C)=CC=N4. InChi Code: InChI=1S/C17H21N5OS/c1-20(2)12-7-8-18-16-13(12)14-15(24-16)17(23)22(11-19-14)21-9-5-3-4-6-10-21/h7-8,11H,3-6,9-10H2,1-2H3. InChi Key: GYWGXEGOXODOQU-UHFFFAOYSA-N.