M TETRABENAZINE (is an active metabolite) | TETRABENAZINE | ATC N07XX06
NERVOUS SYSTEM CNS TREATMENT OF CHOREA ASSOCIATED WITH HUNTINGTON DISEASE INHIBITOR IS BELIEVED TO BE RELATED TO ITS EFFECT AS A REVERSIBLE DEPLETOR OF MONOAMINES (SUCH AS DOPAMINE, SEROTONIN, NOREPINEPHRINE, AND HISTAMINE) FROM NERVE TERMINALS VESICULAR MONOAMINE TRANSPORTER TYPE 2 (VMAT2) (KI=100 NANOMOLAR) | - | Tmax 1 HOUR PPB 61 PERCENT HT 5 HOUR | VESICULAR MONOAMINE TRANSPORTER TYPE 2 (VMAT2) | Synaptic vesicular amine transporter UNIPROT Q05940 SLC18A2 more at DrugCentral | EMA ANSM (in French) Inxight Drugs Dailymed Drugs.com SIDER side effects Chemical Probes Portal ChEMBL BindingDB DrugBank |
TETRABENAZINE (has an active metabolite) | TETRABENAZINE | ATC N07XX06
NERVOUS SYSTEM CNS TREATMENT OF CHOREA ASSOCIATED WITH HUNTINGTON DISEASE INHIBITOR IS BELIEVED TO BE RELATED TO ITS EFFECT AS A REVERSIBLE DEPLETOR OF MONOAMINES (SUCH AS DOPAMINE, SEROTONIN, NOREPINEPHRINE, AND HISTAMINE) FROM NERVE TERMINALS VESICULAR MONOAMINE TRANSPORTER TYPE 2 (VMAT2) (KI=100 NANOMOLAR) | ORAL | F 75 PERCENT PPB 84 PERCENT SOLUBILITY SPARINGLY SOLUBLE IN WATER | VESICULAR MONOAMINE TRANSPORTER TYPE 2 (VMAT2) PDB 8THR (STRUCTURE OF THE HUMAN VESICULAR MONOAMINE TRANSPORTER 2 (VMAT2) BOUND TO TETRABENAZINE IN AN OCCLUDED CONFORMATION) LIGAND CODE = EBZ (link to the list of PDB complexes) Download experimental 3D coordinates of EBZ with added hydrogens | Synaptic vesicular amine transporter UNIPROT Q05940 SLC18A2 more at DrugCentral | EMA ANSM (in French) Inxight Drugs Dailymed Drugs.com SIDER side effects Chemical Probes Portal ChEMBL BindingDB DrugBank |