Tocainide

Tocainide is an antiarrhythmic agent and a derivative of the local anesthetic lidocaine. It inhibits voltage-gated sodium channel 1.4 (Nav1.4) in HEK293 cells expressing the human channel (IC50s = 699 and 182 µM at 0.1 and 10 Hz, respectively). Tocainide reduces the action potential duration at 50% repolarization in isolated dog Purkinje fibers in a concentration-dependent manner. In vivo, tocainide reduces ventricular heart rate and the percent of ectopic beats in a dog model of ventricular tachycardia induced by the cardiac glycoside ouabain (Cay-14319). Tocainide (50 mg/kg) decreases mechanical hyperalgesia in the nerve-injured paw in a rat model of neuropathic pain induced by chronic constriction injury of the sciatic nerve. Formulations containing tocainide have previously been used in the treatment of ventricular arrhythmias.Formal Name: 2-amino-N-(2,6-dimethylphenyl)-propanamide. CAS Number: 41708-72-9. Synonyms: (R,S)-Tocainide, W-36095. Molecular Formula: C11H16N2O. Formula Weight: 192.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Slightly Soluble: 0.1-1 mg/ml, PBS (pH 7.2): Sparingly Soluble: 1-10 mg/ml. SMILES: CC(C(NC1=C(C=CC=C1C)C)=O)N. InChi Code: InChI=1S/C11H16N2O/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12/h4-6,9H,12H2,1-3H3,(H,13,14). InChi Key: BUJAGSGYPOAWEI-UHFFFAOYSA-N.