MRS 5698

MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis[1][2].

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

Adenosine A3 receptor:~3 nM (Ki)

MRS5698 displays higher affinity and selectivity (>3000-fold) agonist A3R vs. other adenosine receptor (ARs) in both human and mouse[1]. MRS5698 (0.1-10 µM; 1 hours) induces a concentration-dependently robust A3R-mediated cAMP reduction in HEK-293T cells permanently expressing the A3R, regardless the illumination condition[3].

MRS5698 (3 nmol/day; intrathecal injection for 25 days) prevents Oxaliplatin-induced mechano-allodynia and hyperalgesia, and attenuates Oxaliplatin-induced NLRP3/IL-1β neuroinflammation[2]. MRS5698 (1 mg/kg; i.p. at days 2, 3 ) reduces the IL-23 induced (IL23 injected in day 0, 1, 3) ear thickness of C57BL/6N mouse during the third and fourth experimental days[3]. Animal Model: Oxaliplatin-induced Male Sprague Dawley rats (200–250 g starting weight)[2] Dosage: 3 nmol/day Administration: Intrathecal injection for 25 days Result: Increased the value of mechanical paw withdrawal threshold in grams (PWT) in rat. Attenuated oxaliplatin-induced expression of NLRP3 and maturation of caspase 1 in the DH-SC. Reduced IL-1β levels in the spinal cord.

[1]. Tosh DK, et al. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 2015;11(3):371-387.

[2]. Wahlman C, et al. Chemotherapy-induced pain is promoted by enhanced spinal adenosine kinase levels through astrocyte-dependent mechanisms. Pain. 2018;159(6):1025-1034.

[3]. López-Cano M, et al. Optical control of adenosine A3 receptor function in psoriasis. Pharmacol Res. 2021 Aug;170:105731.