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A2AR agonist-1 is an agonist of the adenosine A2A receptor and an inhibitor of equilibrative nucleoside transporter 1 (ENT1; Kis = 4.39 and 3.47 µM for the human receptor and guinea pig transporter, respectively).1 It decreases adenosine uptake by 80% in PC12 cells when used at a concentration of 61 µM and increases brain levels of adenosine in a transgenic mouse model of Huntington’s disease when administered at a dose of 20 mg/kg.2 A2AR agonist-1 (0.11 mg/kg) also rescues motor performance and increases survival in a transgenic mouse model of Huntington’s disease.
WARNING This product is not for human or veterinary use.
1. Design and synthesis of novel dual-
2. Targeting ENT1 and adenosine tone for the treatment of Huntington’s disease. Hum. Mol. Genet. 26(3), 467-478 (2017).