(3S,11bS)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one,methanesulfonic acid

Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease[1][2][3].

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monoamine Transporter

Tetrabenazine mesylate (subcutaneous injection, 1-10 mg/kg, once, 10 min) can reduce the aggressive behavior in a dose-dependent manner and the levels of neurotransmitter molecules NE, DA and 5-HT in adult male mice[1]. Tetrabenazine mesylate (intraperitoneal injection, 0-2 mg/kg, once, 30min) has selective effects on movement which can significantly attenuate morphine-induced hypermobility but oral tremors and stereotyped behaviors in male ICR mice[2]. Tetrabenazine mesylate (intraperitoneal injection, 0.25-2 mg/kg, once a week) increases tremulous jaw movement (TJM) in a dose-dependent manner in adult male Sprague-Dawley rat[3]. Animal Model: Adult male MAO A KO or wide type mice aged 1-2 months[1] Dosage: 1-10 mg/kg Administration: Subcutaneous injection; once; 10 min Result: Completely eliminated the aggressive behavior at a concentration of 5 mg/kg and significantly reduced their NE, DA and 5-HT levels. Animal Model: Male ICR mice (10 weeks old)[2] Dosage: 0-2 mg/kg Administration: Intraperitoneal injection; once; 30min Result: Attenuated the subsequent morphine-induced hypermobility after pretreatment with tetrabenazine. Reduced METH-induced increases in locomotion at 1 mg/kg. Animal Model: Adult male Sprague-Dawley rat weighed 350-450 g[3] Dosage: 0.25-2 mg/kg Administration: Intraperitoneal injection; once a week Result: Induced tremulous jaw movement (TJM) significantly at the concentration of 2 mg/kg and more motor impairments with higher doses such as 3-4 mg/kg.

[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.

[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.

[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.