Rasagiline CAS 136236-51-6

Product Name: Rasagiline
Synonyms: (R)-2,3-DIHYDRO-N-2-PROPYNYL-1H-INDEN-1-AMINE;Rasagiline -13C3;Rasagiline;(R)-N-2-Propynyl-1-indanamine;1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-,( 57363782, 57185402,1R);1-Indanamine, N-2-propynyl-,( 57363783, 57185403,R)-;Unii-003N66ts6t;(R)-N-(2-Propynyl)-2,3-dihydroinden-1-aMine
CAS: 136236-51-6
MF: C12H13N
MW: 171.24

Description
Rasagiline is a second-generation, irreversible monoamine oxidase type B (MAO-B) inhibitor that has been launched for the treatment of Parkinson`s disease (PD). Unlike its predecessor selegiline, it is not metabolized to amphetamine derivatives and is, therefore, devoid of the sympathomimetic activity responsible for adverse side effects. Rasagiline is, however, similar to selegiline in the retention of the propargylamine moiety; this essential pharmacophore binds covalently to selectively form an irreversible bond with the flavin adenine dinucleotide portion of the MAO-B enzyme. As an adjunct therapy, rasagiline treats the fluctuations in motor symptoms. The R-enantiomer exhibits 4-times the potency of the S-enantiomer, so the synthetic method begins with the optical resolution of racemic N-benzyl-1-aminoindan using (R,R)-tartaric acid as the resolving agent. Once isolated, the enantiomerically-enriched salt is submitted to hydrogenolysis to afford 1(R)- aminoindane that is subsequently propargylated to provide rasagiline. It is formulated as its mesylate salt, and the recommended dosage of rasagiline is 1 mg/day, with or without levodopa. Entacapone, a catecholamine- O-methyltransferase inhibitor known as an effective add-on therapy for motor fluctuations, was used as a comparator. Rasagiline reduced the time spent in the [off" state while increasing the [on" time.

Uses 5HT4 receptor agonist, peristaltic stimulant