Tetrabenazine

Tetrabenazine is an inhibitor of vesicular monoamine transporter 2 (VMAT2) that is selective over VMAT1 (Kis = 97 and >20,000 nM, respectively, in a serotonin uptake assay). It dose-dependently reduces levels of the monoamines norepinephrine (Cay-16673), dopamine (Cay-21992), and serotonin (5-HT, Cay-14332) in rat brain and has been used to induce depressive-like behavior in animal models. Tetrabenazine (5 mg/kg) improves performance in balance beam and rotarod tests and prevents decreases in the number of striatal medium spiny neurons (MSNs) in a YAC128 transgenic mouse model of Huntington's disease. Formulations containing tetrabenazine have been used in the treatment of chorea associated with Huntington's disease.Formal Name: rel-1,3R,4,6,7,11bR-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-one. CAS Number: 58-46-8. Synonyms: NSC 169886, NSC 172187, Ro 1-9569, TBZ. Molecular Formula: C19H27NO3. Formula Weight: 317.4. Purity: >98% (mixture of enantiomers). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS(pH7.2) (1:2): 0.33 mg/ml, DMSO: 25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 285 nm. SMILES: O=C1[C@@H](CC(C)C)CN2[C@@](C(C=C(OC)C(OC)=C3)=C3CC2)([H])C1. InChi Code: InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3/t14-,16-/m0/s1. InChi Key: MKJIEFSOBYUXJB-HOCLYGCPSA-N.