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MRS2365 (also known as (N)-methanocarba-2MeSADP) is a highly potent and selective small molecule agonist of the Gq-coupled purinergic P2Y1 receptor (P2RY1). Originally synthesized by the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) of the NIH, MRS2365 is widely utilized as a selective pharmacological tool to investigate the role of P2Y1 receptor signaling in platelet aggregation, insulin secretion, and neuroprotection. In vivo, MRS2365 acts as a prodrug that is rapidly dephosphorylated by ectonucleotidases into its active nucleoside metabolite, AST-004 (also known as MRS4322), which acts as an adenosine A1 and A3 receptor agonist. Astrocyte Pharmaceuticals was established to develop this pathway, advancing AST-004 into clinical trials for stroke, traumatic brain injury (TBI), and concussion, while MRS2365 itself remains primarily a research reagent.
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