SCH442416

SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively) . SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain[1][2].

Product Specifications

CAS Number

[316173-57-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/sch442416.html

Purity

99.94

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

Smiles

NC1=NC(N(CCCC2=CC=C(OC)C=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN14

Molecular Formula

C20H19N7O2

Molecular Weight

389.41

Precautions

H302, H315, H319, H335

References & Citations

[1]Todde S, et, al. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A (2A) receptor system using positron emission tomography. J Med Chem. 2000 Nov 16;43 (23) :4359-62.|[2]Moresco RM, et, al. In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416. Eur J Nucl Med Mol Imaging. 2005 Apr;32 (4) :405-13.|[3]Zheng J, et, al. Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am J Physiol Heart Circ Physiol. 2007 Dec;293 (6) :H3685-91.|[4]Maimon N, et, al. Pre-exposure to adenosine, acting via A (2A) receptors on endothelial cells, alters the protein kinase A dependence of adenosine-induced dilation in skeletal muscle resistance arterioles. J Physiol. 2014 Jun 15;592 (12) :2575-90.|[5]Yu J, et, al. A 2A R Antagonists Upregulate Expression of GS and GLAST in Rat Hypoxia Model. Biomed Res Int. 2020 Oct 26;2020:2054293.