ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM[1][2][3].
ZM241385 (1 μM; 24 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly upregulates A2AR mRNA levels[1].ZM241385 (1 μM; 48 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly increases A2AR protein levels[1].
ZM241385 (0.2 μg/mouse, 0.4 μg/mouse; intraperitoneal injection; every day; for 11 weeks; female C57BL/6 WT mice) treatment decreases tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC[4].
References:
[1]. Wang Z, et al. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drugcandidate ZM241385. PLoS One. 2010 Nov 8;5(11):e13883. doi: 10.1371/journal.pone.0013883.
[2]. Linden J, et al. Characterization of human A(2B) adenosine receptors: radioligandbinding, western blotting, and coupling to G(q) in human embryonickidney 293 cells and HMC-1 mast cells. Mol Pharmacol. 1999 Oct;56(4):705-13.
[3]. Poucher SM, et al. The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosinereceptor antagonist. Br J Pharmacol. 1995 Jul;115(6):1096-102.
[4]. Ludwig S, et al. Impact of combination immunochemotherapies on progression of 4NQO-induced murine oral squamous cell carcinoma. Cancer Immunol Immunother. 2019 Jul;68(7):1133-1141.