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Rasagiline Mesylate

Name: Rasagiline Mesylate
Brand: Selleck Chemicals
SKU: S2102
Rating: 5 (1 reviews)

Catalog No.S2102 Synonyms: TVP-1012

For research use only.

Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

CAS No. 161735-79-1

Selleck's Rasagiline Mesylate has been cited by 1 Publication

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MAO Signaling Pathway Map

Biological Activity

Description

Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

Targets

MAO-B ^[1]	MAO-A ^[1]
4.43 nM	412 nM

In vitro

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. ^[1] 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. ^[2] 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. ^[3] 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. ^[4]

In vivo

Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. ^[1] 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. ^[5]

Protocol (from reference)

References

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Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): Saline For best results, use promptly after mixing.	30 mg/mL

Chemical Information

Molecular Weight	267.34
Formula	C₁₂H₁₃N.CH₄O₃S
CAS No.	161735-79-1
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12

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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04841798	Recruiting	Other: [11C]SL25.1188 PET radiotracer	Major Depressive Disorder\|Treatment Resistant Depression	Centre for Addiction and Mental Health	April 15 2021	Not Applicable
NCT01879241	Completed	Drug: Rasagiline\|Drug: Placebo	Amyotrophic Lateral Sclerosis	University of Ulm	June 2013	Phase 2
NCT01652313	Completed	Drug: Rasagiline	Parkinson''s Disease	H. Lundbeck A/S	May 2012	Phase 1
NCT01736891	Completed	Drug: Rasagiline\|Drug: Placebo	Parkinson´s Disease	Chongqing Fortune Pharmaceutical Co. Ltd.\|Beijing Bionovo Medicine Development Co. Ltd.	November 2011	Phase 3
NCT01178047	Terminated	Drug: Rasagiline	Parkinson''s Disease	University of Zurich\|H. Lundbeck A/S	September 2011	Phase 4
NCT01055379	Completed	Drug: Rasagiline\|Drug: Placebo	Depressive Symptoms\|Parkinson''s Disease	Lundbeck Italia S.p.A.\|Teva Branded Pharmaceutical Products R&D Inc.	March 2010	Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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