A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [35S]GTPγS binding Emax[1].
in vivo
In fasted Wistar rats, A3AR modulator 1 (compound 39) has considerably longer in vivo half-life and improved oral bioavailability (3.44 h, 64.0%F at 3 mg/kg; 3.84 h, 61.5%F at 10 mg/kg), indicating substantial oral bioavailability[1].
IC 50
Adenosine A3 receptor
References
[1] Lucas B Fallot, e al. Structure-Activity Studies of 1 H-Imidazo[4,5- c]quinolin-4-amine Derivatives as A3 Adenosine Receptor Positive Allosteric Modulators. J Med Chem. 2022 Nov 24;65(22):15238-15262. DOI:10.1021/acs.jmedchem.2c01170
