Tetrabenazine (Racemate)

Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome^[1][2][3]. In Vitro:Tetrabenazine Racemate reversibly inhibits human VMAT2 with a K_i of ~100 nM, reducing monoamine uptake into synaptic vesicles and depleting presynaptic monoamine stores^[1].
Tetrabenazine Racemate inhibits dopamine D2 receptors in striatal membranes with a K_i of ~2.1 μM^[1].
Tetrabenazine Racemate (0.3-10.0 μg/mL; 4 h) releases serotonin from rabbit blood platelets in vitro in a concentration-dependent manner^[3].
Tetrabenazine Racemate (5-20 mg/L) is 60% bound to nondiffusible components of rabbit plasma^[3]. In Vivo:Tetrabenazine Racemate provides partial neuroprotection in a transgenic HD mouse model of Glutamate-induced striatal neurodegeneration^[1].
Tetrabenazine Racemate (7 days) causes irreversible locomotor changes and substantia nigra pars compacta neuronal damage in healthy rats^[1].
Tetrabenazine Racemate (50-150 mg/kg; i.v.; daily for 3-9 days) exhibits short-lived, central nervous system-selective Reserpine (HY-N0480)-like effects in rabbits^[3].