Tiagabine (hydrochloride)

Tiagabine is an inhibitor of GABA transporter 1 (GAT-1, IC50 = 49 nM for GAT-1 expressed in CHO cells). It inhibits seizures induced by DMCM in mice (ED50 = 1.2 mg/kg, i.p.). Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin (Cay-10008346) to delay pain responses in mice in the hot plate test. Formulations containing tiagabine have been used as adjunctive therapies in the treatment of partial seizures.Formal Name: (3R)-1-[4,4-bis(3-methyl-2-thienyl)-3-buten-1-yl]-3-piperidinecarboxylic acid, monohydrochloride. CAS Number: 145821-59-6. Synonyms: ABT-569. Molecular Formula: C20H25NO2S2 . HCl. Formula Weight: 412.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 256 nm. SMILES: OC([C@@H]1CCCN(CC/C=C(C2=C(C)C=CS2)\C3=C(C)C=CS3)C1)=O.Cl. InChi Code: InChI=1S/C20H25NO2S2.ClH/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23,/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23),1H/t16-,/m1./s1. InChi Key: YUKARLAABCGMCN-PKLMIRHRSA-N.