| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.048 nM (hA2AR), 0.5 nM (rA2AR) | ||||||||||||
| Invitro | SCH442416 is selective for A2AR (Ki=0.50 nM) in rat striatal membranes over A1R and A3R (Ki=1815 and >10000, respectively)[1].SCH442416 (0.1-10 μM) increases the glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) proteins expression of Müller cells in Group 1 μM[5]. | ||||||||||||
| In Vivo | SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury[3].SCH-442416 (1 μM•2μL; i.v.) increases the GS and GLAST protein expression in rats[5].SCH442416 (1 μM) significantly attenuates the adenosine-induced dilation (from 15.3 to 5.6 μm)[4]. | ||||||||||||
| Name | SCH442416 | ||||||||||||
| CAS | 316173-57-6 | ||||||||||||
| Formula | C20H19N7O2 | ||||||||||||
| Molar Mass | 389.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |