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First P2Y12 Receptor Antagonist Available from Sigma-RBI
2,2-Dimethyl-propionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-
2-(2,2-dimethyl-propionyloxymethyl)-propyl ester
Prod. No. M5942
The surface receptors for extracellular nucleotides, both purine and pyrimidine, are called P2 receptors. P2 receptors are divided into two categories based on molecular structure and signal transduction mechanisms: P2Y (G-protein coupled receptors) and P2X (ligand-gated ion channels) (1). These receptor subtypes are found in the central and peripheral nervous system, the cardiovascular system, the endocrine system, lungs, intestines, muscle, and the immune system (2). Twelve P2Y receptor subtypes have been identified: P2Y1-12. Each P2Y receptor binds to a single heterotrimeric G protein (typically Gq/11), although P2Y12 couples to GI. Endogenous P2Y receptors can activate phopholipases A2, C, and D MEP/MAP kinase, Rho-dependent kinase and tyrosine kinase, as well as coupling both positively and negatively to adenylyl cyclase (1). In the cardiovascular system, ADP that is released from platelets and endothelial cells can induce aggregation of platelets by acting at P2Y1 and P2Y12 receptors; thus, antagonists of these subtypes may display antithrombotic properties (2).
Features & Benefits
MRS 2395 is one of the first identified antagonists of P2Y12 receptors, giving researchers a new tool in studying the function of this receptor subtype as well as its role in various physiological functions.
- MRS 2395 inhibited ADP-induced aggregation in rat platelets with KI = 3.6 7 µM (2).
- MRS 2395 was found to antagonize ADP-induced inhibition of cAMP in rat and human platelets in the presence of PGE1, (IC50 = 7 µM and 30 µM respectively), without affecting P2Y1 receptor-induced PLC activity in transfected astrocytoma cells (2).
| Related P2 Receptor Antagonists available from Sigma-RBI |
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| Product # |
Product Name |
Selectivity |
| D6938 |
Diinosine pentaphosphate pentasodium salt |
P2X1/P2X3 |
| M7684 |
MRS 2159 |
P2X1 |
| M3808 |
MRS 2179 |
P2Y1, competitive |
| N8652 |
NF 023 |
P2X1, potent, selective |
| P2738 |
PPNDS |
P2X1 |
| P-178 |
PPADS |
P2 |
| R-115 |
Reactive Blue 2 |
P2Y |
| T4193 |
TNP-ATP |
P2X2/3 |
References
- The Sigma-RBI Handbook of Receptor Classification and Signal Transduction, 4th edition, Keith J. Watling, ed., pg. 64 (2001).
- Xu, B et al., Acyclic analogues of adensoine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple 4 pathways of inhibition of platelet aggregation, J. Med. Chem., 45, 5694-5709 (2002).
For more information about calcium channel modulators, please visit The Sigma-RBI Handbook of Receptor Classification and Signal Transduction.
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