2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. Monoamine Transporter Dopamine Receptor
  4. Tetrabenazine mesylate

Tetrabenazine mesylate  (Synonyms: Ro 1-9569 mesylate)

Cat. No.: HY-B0590E
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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.

For research use only. We do not sell to patients.

Tetrabenazine mesylate

Tetrabenazine mesylate Chemical Structure

CAS No. : 804-53-5

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Tetrabenazine mesylate Related Antibodies

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Description

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].

IC50 & Target

D2 Receptor

~2.1 μM (Ki)

In Vitro

Tetrabenazine mesylate reversibly inhibits human VMAT2 with a Ki of ~100 nM, reducing monoamine uptake into synaptic vesicles and depleting presynaptic monoamine stores[1].
Tetrabenazine mesylate inhibits dopamine D2 receptors in striatal membranes with a Ki of ~2.1 μM[1].
Tetrabenazine (0.3-10.0 μg/mL; 4 h) mesylate releases serotonin from rabbit blood platelets in vitro in a concentration-dependent manner[3].
Tetrabenazine (5-20 mg/L) mesylate is 60% bound to nondiffusible components of rabbit plasma[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tetrabenazine mesylate Related Antibodies
In Vivo

Tetrabenazine mesylate provides partial neuroprotection in a transgenic HD mouse model of Glutamate-induced striatal neurodegeneration[1].
Tetrabenazine (7 days) mesylate causes irreversible locomotor changes and substantia nigra pars compacta neuronal damage in healthy rats[1].
Tetrabenazine (50-150 mg/kg; i.v.; daily for 3-9 days) mesylate exhibits short-lived, central nervous system-selective Reserpine (HY-N0480)-like effects in rabbits[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: New Zealand White male (~2 kg)[3]
Dosage: 50 mg/kg; 150 mg/kg
Administration: i.v.; daily for 3, 7, 9 days
Result: Decreased brain serotonin to ~50% of normal within 1 hour, remained at this level for several hours, and returned to near normal by 18-24 hours.
Declined brain norepinephrine to ~15% of normal over 4 hours, and returned to ~70% of normal by 24 hours.
Did not measurably affect peripheral serotonin in blood platelets and small intestine, and norepinephrine in heart.
Caused <10% depletion of adrenal catecholamines at 4 hours and ~40% depletion at 24 hours.
Reduced plasma drug levels to <3 μg/mL by 6 hours, and made them undetectable by 24 hours.
Reached brain drug levels of ~45 μg/g within 10 minutes, declined to ~1.3 μg/g by 6 hours, and made them undetectable by 24 hours.
Failed to affect intestinal/platelet serotonin or heart norepinephrine, but caused 50% depletion of adrenal catecholamines by the end of infusion with single 150 mg/kg i.v. dose.
Showed no drug accumulation in plasma or tissues 24 hours after the last dose with repeated 50 mg/kg daily i.v. doses.
Clinical Trial
Molecular Weight

413.53

Formula

C20H31NO6S
CAS No.
SMILES

CS(=O)(O)=O.O=C1[C@@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@]2([H])C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tetrabenazine mesylate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tetrabenazine804-53-5Ro 1-9569Monoamine TransporterDopamine Receptorsubstantia nigramonoamineTourette’s syndromerabbit blood plateletscerebrospinal fluid homovanillic acidstriatal membraneshuman dopamine D2 receptortransgenic HD mouse modelVMAT2Huntington’s diseaseInhibitorinhibitorinhibit

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