779323-43-2

Usage

Uses

Used in Pharmaceutical Industry:
MRS 2500 tetraammonium salt is used as a highly potent and selective antagonist for the platelet P2Y1 receptor. Its application is primarily focused on inhibiting ADP-induced aggregation of human platelets, which can be beneficial in the treatment and management of various blood clotting disorders and cardiovascular diseases.
Used in Research and Development:
In addition to its pharmaceutical applications, MRS 2500 tetraammonium salt can also be utilized in research and development settings. It can serve as a valuable tool for studying the role of the P2Y1 receptor in platelet function and related physiological processes. This may lead to a better understanding of the underlying mechanisms involved in blood clotting and the development of novel therapeutic strategies for related conditions.
Used in Drug Delivery Systems:
Similar to gallotannin, MRS 2500 tetraammonium salt could potentially be incorporated into drug delivery systems to enhance its bioavailability and therapeutic outcomes. By employing various organic and metallic nanoparticles as carriers, the compound's delivery, efficacy, and targeting capabilities could be improved, allowing for more effective treatment of conditions related to platelet aggregation and blood clotting.

Biological Activity

Highly potent and selective antagonist of the platelet P2Y 1 receptor (K i = 0.78 nM). Inhibits ADP-induced aggregation of human platelets with an IC 50 value of 0.95 nM. Prevents thrombus formation in vivo .

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Relevant academic research and scientific papers

Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor

Activation of the P2Y1 nucleotide receptor in platelets by ADP causes changes in shape and aggregation, mediated by activation of phospholipase C (PLC). Recently, MRS2500 (2-iodo-N6-methyl-(N)-methanocarba- 2′-deoxyadenosine-3′,5′-bi

2-Substitution of Adenine Nucleotide Analogues containing a Bicyclo[3.1.0]hexane Ring System Locked in a Northern Conformation: Enhanced Potency as P2Y1 Receptor Antagonists

Preference for the northern (N) ring conformation of the ribose moiety of adenine nucleotide 3′,5′-bisphosphate antagonists of P2Y 1 receptors was established by using a ring-constrained methanocarba (a bicyclo[3.1.0]hexane) ring as a ribose su