804-53-5
Chemical Structure
Tetrabenazine mesylate
Synonym(s): Ro 1-9569 mesylate
- CAS No.: 804-53-5
- Formula:C20H31NO6S
- Molecular Weight:413.53
IUPAC Name: (3S,11bS)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one methanesulfonate
InChIKey: RHDADYXNUCMTQG-DMLYUBSXSA-N
SMILES: CS(=O)(O)=O.O=C1[C@@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@]2([H])C1
Biological Activity: Tetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome[1][2][3].
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Tetrabenazine mesylate | Tetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome. | |||||||||||||||||||||
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- [1]. J C Shih, et al. Ketanserin and tetrabenazine abolish aggression in mice lacking monoamine oxidase A. Brain Res. 1999 Jul 24;835(2):104-12. [Content Brief]
- [2]. Nobue Kitanaka, et al. Tetrabenazine, a vesicular monoamine transporter-2 inhibitor, attenuates morphine-induced hyperlocomotion in mice through alteration of dopamine and 5-hydroxytryptamine turnover in the cerebral cortex. Pharmacol Biochem Behav. 2018 Sep;172:9-16. doi: 10.1016/j.pbb.2018.07.002. Epub 2018 Jul 12. [Content Brief]
- [3]. S J Podurgiel, et al. The vesicular monoamine transporter (VMAT-2) inhibitor tetrabenazine induces tremulous jaw movements in rodents: implications for pharmacological models of parkinsonian tremor. Neuroscience. 2013 Oct 10;250:507-19. doi: 10.1016/j.neuroscience.2013.07.008. Epub 2013 Jul 15. [Content Brief]
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