Tozadenant

Names

[ Name ]:
Tozadenant

[Synonym ]:
4-hydroxy-n-(4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl)-4-methyl-1-piperidinecarboxamide
4-hydroxy-4-methyl-piperidine-1-carboxylic acid(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide
Tozadenant
SYN-115
4-Hydroxy-N-[4-methoxy-7-(4-morpholinyl)-1,3-benzothiazol-2-yl]-4-methyl-1-piperidinecarboxamide
4-Hydroxy-N-(4-methoxy-7-morpholinobenzo(d)thiazol-2-yl)-4-methylpiperidine-1-carboxamide
Tozadenant (USAN)
1-Piperidinecarboxamide, 4-hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl-
4-Hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl-1-piperidinecarboxamide

Biological Activity

[Description]:

Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

Research Areas >> Neurological Disease

[Target]

Ki: 6 nM (Rhesus A2A), 11.5 nM (Human A2A)

[In Vivo]

18F-MNI-444 regional uptake is consistent with A2A receptor distribution in the brain. Selectivity is demonstrated by dose-dependent blocking by tozadenant (1.5, 10.5 mg/kg) and preladenant[1].

[References]

[1]. Olivier Barret, et al. Adenosine 2A Receptor Occupancy by Tozadenant and Preladenant in Rhesus Monkeys. J Nucl Med. 2014 Oct;55(10):1712-8.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₁₉H₂₆N₄O₄S

[ Molecular Weight ]:
406.499

[ Exact Mass ]:
406.167480

[ PSA ]:
118.89000

[ LogP ]:
0.43

[ Index of Refraction ]:
1.662

Safety Information

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%