Drug intelligence / Profile preview

MRS5698

Development stage
Preclinical
Lead developer
National Institute of Diabetes and Digestive and Kidney Diseases
Modality
Small Molecules
Administration
Intraperitoneal, Intrathecal, Oral, Subcutaneous
01

Overview

MRS5698 is a highly selective, orally bioavailable small molecule agonist of the adenosine A3 receptor (A3AR). It was developed through a research collaboration involving the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK/NIH), Saint Louis University, and Primetime Life Sciences. MRS5698 exhibits high affinity for both human and rodent A3AR (Ki ~3 nM) with greater than 1000-fold selectivity over other adenosine receptor subtypes (A1, A2A, and A2B). It has been investigated preclinically for the treatment of chronic neuropathic pain, where it reverses mechanoallodynia and attenuates neuroinflammation without inducing tolerance, as well as for psoriasis.

Other names
(1S,2R,3S,4R,5S)-4-(6-((3-chlorobenzyl)amino)-2-((3,4-difluorophenyl)ethynyl)-9H-purin-9-yl)-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamide(1S,2R,3S,4R,5S)-4-[6-[[(3-chlorophenyl)methyl]amino]-2-[2-(3,4-difluorophenyl)ethynyl]-9H-purin-9-yl]-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamideMRS 5698MRS5698MRS-5698
02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)ADORA3 (Adenosine A3 receptor)

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