| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 100mg | 电议 |
Tetrabenazine is the only US Food and Drug Administration-approved drug for Huntington's disease, indicated for treatment of chorea associated with Huntington's disease.
Cell lines | Neuro-2a neuroblastoma cell line |
Preparation Method | Neuro-2a cells were incubated for 24h with tetrabenazine solution, tetrabenazine loaded nanoemulsion and placebo. |
Reaction Conditions | 2.4/4.8/9.6 ng/mL Tetrabenazine for 24h |
Applications | Tetrabenazine loaded nanoemulsion showed 100.00±1.23%, 100.00±2.01% and 100.00±2.09% cell viability when treated at the dose of 4.8ng/mL, 2.4ng/mL and 9.6ng/Ml. |
Animal models | Wistar rats (200-250g) of age 11-12 weeks |
Preparation Method | Tetrabenazine solution was administered intravenously to group 1 (dose 1.25mg/day dissolved in 1mL of normal saline solution). Second group of animals received tetrabenazine nanoemulsion administered intranasally (dose equivalent to 1.25mg/day). Dosage volume administered to each nostril was 25μL. Rats were sacrificed humanely by cervical dislocation method at different time intervals (0.5, 1, 6 and 12h) after collecting blood from retino-orbital vein in precoated EDTA tube. |
Dosage form | 1.25mg/day Tetrabenazine for 0.5!c1!c6!c12h |
Applications | The superiority of tetrabenazine nanoemulsion for delivering of tetrabenazine via intranasal route bypassing BBB. |
| 产品描述 | Tetrabenazine is the only US Food and Drug Administration-approved drug for Huntington's disease, indicated for treatment of chorea associated with Huntington's disease[1,3,4]. It reversibly inhibits central vesicular monoamine transporter (VMAT) transporter type 2 which acts on the various monoaminergic systems in the brain, e.g., dopamine, serotonin and noradrenaline[5]Tetrabenazine binds predominately to VMAT2 and has been shown to reversibly inhibit monoamine uptake in pre-synaptic vesicles, resulting in monoamine depletion of serotonin, dopamine, and nor-epinephrine[6]thereby reducing chorea[7]. In Neuro-2a neuroblastoma cell line, Tetrabenazine loaded nanoemulsion showed 100.00±1.23%, 100.00±2.01% and 100.00±2.09% cell viability when treated at the dose of 4.8ng/mL, 2.4ng/mL and 9.6ng/Ml[2]. When used bovine chromaffin cells (BCCs) challenged with repeated pulses of high K+ Upon repeated K+ pulsing, the exocytotic catecholamine release responses were gradually decaying. However, when cells were exposed to tetrabenazine, responses were mildly augmented and decay rate delayed[8]. In rat, The superiority of tetrabenazine nanoemulsion for delivering of tetrabenazine via intranasal route bypassing BBB[2]. In mice, Cold-water immersion-induced acute stress diminished the locomotor activity, exploratory behaviour, motor activity and social behaviour along with increase in the plasma corticosterone levels. Administration of tetrabenazine (1 and 2 mg/kg, i.p.), abolished the acute stress-induced behavioural and biochemical changes in a dose-dependent manner[9]. References: |
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