Repositioning Candidate Details
| Candidate ID: | R0429 |
| Source ID: | DB04844 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Tetrabenazine |
| Synonyms: | |
| Molecular Formula: | C19H27NO3 |
| SMILES: | COC1=C(OC)C=C2C3CC(=O)C(CC(C)C)CN3CCC2=C1 |
| Structure: |
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| DrugBank Description: | A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders. It is a monoamine depletor and used as symptomatic treatment of chorea associated with Huntington's disease. FDA approved on August 15, 2008. |
| CAS Number: | 58-46-8 |
| Molecular Weight: | 317.4226 |
| DrugBank Indication: | Treatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesia |
| DrugBank Pharmacology: | Prolongation of the QTc interval has been observed at doses of 50 mg. In rats, it has been observed that tetrabenazine or its metabolites bind to melanin-containing tissues such as the eyes and skin. After a single oral dose of radiolabeled tetrabenazine, radioactivity was still detected in eye and fur at 21 days post dosing. |
| DrugBank MoA: | Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor (Ki = 100 nM). It acts within the basal ganglia and promotes depletion of monoamine neurotransmitters serotonin, norepinephrine, and dopamine from stores. It also decreases uptake into synaptic vesicles. Dopamine is required for fine motor movement, so the inhibition of its transmission is efficacious for hyperkinetic movement. Tetrabenazine exhibits weak in vitro binding affinity at the dopamine D2 receptor (Ki = 2100 nM). |
| Targets: | Synaptic vesicular amine transporter; Dopamine D2 receptor |
| Inclusion Criteria: |
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