804-53-5

804-53-5 structure

Name: (3S,11bS)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one,methanesulfonic acid
Chemical Name: (3S,11bS)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one,methanesulfonic acid
CAS Number: 804-53-5
Molecular Formula: C₂₀H₃₁NO₆S
Molecular Weight: 413.52800
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Monoamine Transporter
Create Date: 2017-06-25 17:12:25
Modify Date: 2024-04-02 14:53:21
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].

Name	(3S,11bS)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one,methanesulfonic acid
Synonyms	Tetrabenazine methanesulfonate UNII-5X57I1N37U

Description	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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Monoamine Transporter
In Vivo	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.
References	[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.

Molecular Formula	C₂₀H₃₁NO₆S
Molecular Weight	413.52800
Exact Mass	413.18700
PSA	101.52000
LogP	3.76080

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