product name Rasagiline Mesylate
Description: Rasagiline Mesylate (also known as TVP-1012) is a novel, selective irreversible MAO-B inhibitor for the treatment of idiopathic Parkinsons disease. It displays anti-Parkinsonian activity, exhibits neuroprotective and antiapoptotic activity against several neurotoxins in cell culture. Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro.
References: Br J Pharmacol. 2001 Jan;132(2):500-6; Eur J Pharmacol. 1999 Feb 5;366(2-3):127-35.
267.34
Formula
C12H13N.CH4O3S
CAS No.
161735-79-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (198.2 mM)
Water: 53 mg/mL (198.2 mM)
Ethanol: 53 mg/mL (198.2 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
TVP-1012
other peoduct :
| In Vitro |
In vitro activity: Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro. Rasagiline prevents nuclear accumulation of GAPDH induced by N-methyl(R) salsolinol in SH-SY5Y cells. Rasagiline prevents the collapse in ΔΨm, and following apoptotic process, which indicates that mitochondria may determine the survival and death of the cells. Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and NGF withdrawal in partially neuronally differentiated PC12 cells and prevents the fall in mitochondrial membrane potential, the first step in cell death. Rasagiline is metabolized to its major metabolite aminoindan, selegiline gives rise to L-methamphetamine. Rasagiline directly activates PKC-MAP kinase pathway by a concentration and time dependent phosphorylation of p42 and p44 MAP kinase. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. Rasagiline (0.2 mg/kg and 1 mg/kg) accelerates the recovery of motor function and spatial memory and reduces the cerebral oedema by about 40-50% in the mouse. |
| Animal model | |
| Formulation & Dosage | |
| References | Br J Pharmacol. 2001 Jan;132(2):500-6; Eur J Pharmacol. 1999 Feb 5;366(2-3):127-35. |
