A3885-50mg | Tozadenant [870070-55-6] Clinisciences

Tozadenant (SYN115) is an orally active, selective adenosine A2A receptor antagonist.

In animal models of Parkinson’s disease, tozadenant improves motor neuron function.

Tozadenant (60 mg twice daily) was not associated with a signi cant reduction in o -time, and tozadenant (240 mg twice daily) was associated with an increased rate of discontinuation because of adverse events (17 of 84 patients [20%]). Tozadenant at dose of 120 or 180 mg twice daily was e ective at reducing o -time and was generally well tolerated. Further investigation of tozadenant treatment in phase 3 trials is guaranteed. Perfusion MRI showed that tozadenant induced highly signi cant suppressed in regional cerebral blood ow, with the most important decreases occurring in bilateral thalami.

Reference:
Hauser RA, Olanow CW, Kieburtz KD et al. Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76.

Storage	Store at -20°C
M.Wt	406.5
Cas No.	870070-55-6
Formula	C₁₉H₂₆N₄O₄S
Synonyms	SYN-115;SYN115;SYN 115
Solubility	insoluble in EtOH; insoluble in H2O; ≥20.35 mg/mL in DMSO
Chemical Name	4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide
SDF	Download SDF
Canonical SMILES	CC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Human experiment [1]:
Patients	Patients with Parkinson’s disease.
Dosage form	60, 120, 180, or 240 mg twice daily for 12 weeks.
Applications	Tozadenant increases mean daily total on-time and improved total UPDRS scores for parts I-III in the combined tozadenant 120 mg twice-daily and 180 mg twice-daily group and in the 120 mg twice-daily group. Also, tozadenant significantly improved CGI-S and CGI-I scores.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Hauser RA, Olanow CW, Kieburtz KD, et al. Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol,2014, 13(8): 767-776.

Description	Tozadenant is an antagonist of adenosine A2A receptor.
Targets	adenosine A2A receptor
IC50

Purity = 99.46%

Tozadenant [870070-55-6]

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Background

Chemical Properties

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Biological Activity

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