Catalog No.S5795 Synonyms: TVP-1012
Molecular Weight(MW): 171.24
Rasagiline is a novel selective and irreversible MAO-B propargylamine inhibitor with in vitro IC50s of 4.43 nM and 412 nM for MAO-B and MAO-A, respectively.
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|Description||Rasagiline is a novel selective and irreversible MAO-B propargylamine inhibitor with in vitro IC50s of 4.43 nM and 412 nM for MAO-B and MAO-A, respectively.|
Rasagiline is a highly selective and potent propargylamine inhibitor of monoamine oxidase (MAO) type B. Like other similar propargylamine inhibitors, rasagiline binds covalently to the N5 nitrogen of the flavin residue of MAO, resulting in irreversible inactivation of the enzyme. Rasagiline possesses a similar degree of selectivity to selegiline for inhibition of MAO-B as compared with MAO-A, in rat hepatic and brain tissue both in vivo and in vitro. Both inhibitors will inhibit the A form of the enzyme at higher doses.
|In vivo||Rasagiline is well absorbed after oral administration and readily crosses the BBB. The oral bioavailability of rasagiline is 35%, it reaches Tmax after 0.5-1 hours and its half-life is 1.5-3.5 hours. It exerts linear absorption at doses of 1-10 mg/day. Rasagiline undergoes extensive hepatic metabolism primarily by cytochrome P450 type 1A2 (CYP1A2). Plasma albumin binding is considered to be 60%-70%.|
|In vitro||DMSO||34 mg/mL (198.55 mM)|
|Ethanol||34 mg/mL (198.55 mM)|
|Water||4 mg/mL (23.35 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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 Pharmaceutical Industries||March 2010||Phase 4|
|NCT00203164||Completed||Drug: rasagiline mesylate||Parkinson''s Disease||Teva Pharmaceutical Industries||May 2002||Phase 3|
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