(1R)-N-prop-2-yn-1-yl-2,3-dihydro-1H-inden-1-amine methanesulfonate
Rasagiline mesylate
CAS: 161735-79-1
Molecular Formula: C13H17NO3S
(1R)-N-prop-2-yn-1-yl-2,3-dihydro-1H-inden-1-amine methanesulfonate - Names and Identifiers
| Name | Rasagiline mesylate |
| Synonyms | CS-289 Agilect Rasagiline mesylate R-(+)-Rasagiline mesylate (R)-N-2-Propynyl-1-indanamine Mesylate (1R)-2,3-Dihydro-N-2-propyn-1-yl-1H-inden-1-amine Mesylate (1R)-2,3-Dihydro-N-2-propynyl-1H-inden-1-amine methanesulfonate N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine methanesulfonate (1R)-N-prop-2-yn-1-yl-2,3-dihydro-1H-inden-1-amine methanesulfonate |
| CAS | 161735-79-1 |
| EINECS | 694-423-3 |
| InChI | InChI=1/C12H13N.CH4O3S/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12;1-5(2,3)4/h1,3-6,12-13H,7-9H2;1H3,(H,2,3,4)/t12-;/m1./s1 |
(1R)-N-prop-2-yn-1-yl-2,3-dihydro-1H-inden-1-amine methanesulfonate - Physico-chemical Properties
| Molecular Formula | C13H17NO3S |
| Molar Mass | 267.34398 |
| Melting Point | 155-158°C |
| Boling Point | 305.5°C at 760 mmHg |
| Flash Point | 146.8°C |
| Solubility | DMSO 53 mg/mL Water 53 mg/mL Ethanol 53 mg/mL |
| Vapor Presure | 0.000816mmHg at 25°C |
| Appearance | White powder |
| Color | white to tan |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO, distilled water or ethanol may be stored at -20°C for up to 1 month. |
| MDL | MFCD08460604 |
| In vitro study | Rasagiline inhibited rat brain tissue maotype A and Type B, and IC50 was 4.43 nM and 412 nM, respectively. After acute and chronic administration, Rasagiline inhibited the MAO-B of rat brain and liver 3 to 15 times more than selegiline, but the potency was similar in vitro. In SH-SY5Y cells, Rasagiline prevents nuclear accumulation of N-methyl (R)salsolinol-induced GAPDH. Rasagiline prevents the decay of the mitochondrial membrane potential that accompanies the process of apoptosis, suggesting that Mitochondria determine whether a cell lives or dies. Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and growth factor withdrawal and prevents the decline of mitochondrial membrane potential in partially neurodifferentiated PC12 cells, this is the first step in cell death. Rasagiline is metabolized to its main metabolite, aminoindan, and selegiline produces methamphetamine. Rasagiline directly activates the protein kinase C- MAP kinase pathway by concentration-and time-dependent phosphorylation of P42 and P44 MAP kinases. |
| In vivo study | Rasagiline inhibited MAO in isolated 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 brain edema by about 40-50% in mice. |
(1R)-N-prop-2-yn-1-yl-2,3-dihydro-1H-inden-1-amine methanesulfonate - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| HS Code | 29214990 |
(1R)-N-prop-2-yn-1-yl-2,3-dihydro-1H-inden-1-amine methanesulfonate - Reference Information
| Parkinson's disease drug | rasagiline mesylate was developed by Israel Teva pharmaceutical industry company. it was first approved by the European drug administration (EMA) on February 21, 2005 and approved by the U.S. food and drug administration (FDA) on may 16, 2006. It is suitable for single treatment of patients with primary Parkinson's disease (without levodopa), and as an adjunct to levodopa for Parkinson's patients with end-dose fluctuation. Rasagiline mesylate is an irreversible monoamine oxidase inhibitor. By selectively inhibiting monoamine oxidase, it can reduce the decomposition of dopamine and increase the extracellular level of dopamine in the striatum of the brain. The increased dopamine level can reduce Parkinson's disease symptoms. Compared with selegiline (the first generation of monoamine oxidase inhibitors, including Skinin, mididopyrion, Jinsiping), rasagiline mesylate has a strong inhibitory effect of 5-10 times, and it is effective for long-term use of dopa. Patients with declining efficacy also have an improvement effect. In addition, the metabolite of rasagiline is an inactive non-amphetamine substance with few side effects. More importantly, unlike other anti-Parkinson's drugs, rasagiline mesylate also has neuroprotective effects. Combined therapy can optimize the therapeutic effect of levodopa, further effectively control symptoms and reduce motor complications. According to 2017 US IMS data, among the world's top 500 best-selling drug markets, the anti-Parkinson's treatment market was US $2.056 billion, up 3.73% from the previous year. |
| pharmacological action | pharmacological mechanism of rasagiline: rasagiline is a potent, highly selective and irreversible monoamine oxidase-B inhibitor, which can inhibit dopamine degradation, increase dopamine accumulation, promote dopamine release and improve clinical symptoms of PD patients. It has a new chemical structure. The purpose of the new chemical structure is to improve the deficiency of primary MAO-B inhibitor treatment. selegiline is a first-generation MAO-B inhibitor. its metabolites include amphetamine derivatives, which can cause adverse reactions, such as affecting patients' sleep. The metabolites of rasagiline do not contain amphetamine derivatives. In vitro studies have confirmed that the metabolite of rasagiline, aminoindan, has a neuroprotective effect. The combination of rasagiline and MAO-B is highly selective. It is characterized by maintaining a distance between the aromatic ring and the N-propargyl terminal in the structure. The distance between the two carbon units, and the effective group N-propargiline group triple The bond is essential to maintain the irreversibility of rasagiline. Irreversible effect means that the effect lasts, so it may provide continuous dopaminergic stimulation (continuous dopaminergicstimulation, CDS). This is the basis for the realization of the once-daily administration method; the data shows that the pharmacokinetic half-life of rasagiline has nothing to do with the pharmacodynamic half-life, and the clinical efficacy lasts up to 24 hours. |
| biological activity | Rasagiline Mesylate (TVP-1012) is a new type of MAO-B inhibitor used to treat sudden Parkinson's disease. |
| Target | Value |
| MAO-B | 4.43 nM |
| MAO-A | 412 nM |
Last Update：2024-04-09 21:11:58
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