Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide increases neostriatal dopamine concentration. In addition, safinamide is voltage-dependent sodium and calcium channel blocker. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals. Safinamide significantly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide has a high oral bioavailability (80–92%), is rapidly absorbed in plasma after reaching the peak within 0.5–2 hours declines, with a terminal half-life of about 3, 7, and 13 hours in mice, rats, and monkeys, respectively. Safinamide is currently in a Phase II clinical trial.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL
Water 80 mg/mL
|Related Monoamine Oxidase Products|
Radafaxine Hcl(BW-306U; GW-353162A) is a potent metabolite of bupropion; selective for inhibiting the reuptake of norepinephrine over dopamine; DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
Pargyline hydrochloride is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension.
Iproniazid is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class.
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