ArticlePharmacological research2010
Quantification of recombinant and platelet P2Y(1) receptors utilizing a [(125)I]-labeled high-affinity antagonist 2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([(125)I]MRS2500).
Article in Pharmacological research, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 33 citations in OpenAlex.
- Advances in nucleotide-based P2Y₁ antagonism: implications for cardiovascular therapeutics.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Pharmacological characterization of P2Y receptor subtypes - an update.Purinergic signalling · 2024Review
- ADP-Mediated Upregulation of Expression of CD62P on Human Platelets Is Critically Dependent on Co-Activation of P2Y1 and P2Y12 Receptors.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Update of P2Y receptor pharmacology: IUPHAR Review 27.British journal of pharmacology · 2020Review
- A MATHEMATICAL MODEL OF PLATELET AGGREGATION IN AN EXTRAVASCULAR INJURY UNDER FLOW.Multiscale modeling & simulation : a SIAM interdisciplinary journal · 2020Article
- Platelets at the Vascular Interface.Research and practice in thrombosis and haemostasis · 2018Article
- Ligand binding to a G protein-coupled receptor captured in a mass spectrometer.Science advances · 2017Article
- Blood cells: an historical account of the roles of purinergic signalling.Purinergic signalling · 2015Review
- Platelet biology and receptor pathways.Journal of cardiovascular translational research · 2013Review
- The platelet P2Y(12) receptor under normal and pathological conditions. Assessment with the radiolabeled selective antagonist [(3)H]PSB-0413.Purinergic signalling · 2013Article
- P2Y(12) receptors in platelets and other hematopoietic and non-hematopoietic cells.Purinergic signalling · 2012Review
- Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.Bioorganic & medicinal chemistry · 2012Article
- A platelet target for venous thrombosis? P2Y1 deletion or antagonism protects mice from vena cava thrombosis.Journal of thrombosis and thrombolysis · 2012Article
- P2 receptors and platelet function.Purinergic signalling · 2011Article
- Pharmacochemistry of the platelet purinergic receptors.Purinergic signalling · 2011Article
- Ser352 and Ser354 in the carboxyl terminus of the human P2Y(1) receptor are required for agonist-promoted phosphorylation and internalization in MDCK cells.British journal of pharmacology · 2011Article
- Functionalized congeners of P2Y1 receptor antagonists: 2-alkynyl (N)-methanocarba 2'-deoxyadenosine 3',5'-bisphosphate analogues and conjugation to a polyamidoamine (PAMAM) dendrimer carrier.Bioconjugate chemistry · 2010Article
- Activation of distinct P2Y receptor subtypes stimulates insulin secretion in MIN6 mouse pancreatic beta cells.Biochemical pharmacology · 2010Article
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Authors and funding
6 authors at 6 institutions in 2 countries.
Funding
Abstract
The ADP-activated P2Y(1) receptor is broadly expressed and plays a crucial role in ADP-promoted platelet aggregation. We previously synthesized 2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate (MRS2500), as a selective, high-affinity, competitive antagonist of this receptor. Here we report utilization of a trimethylstannyl precursor molecule for the multi-step radiochemical synthesis of a [(125)I]-labeled form of MRS2500. [(125)I]MRS2500 bound selectively to Sf9 insect cell membranes expressing the human P2Y(1) receptor but did not specifically bind to membranes isolated from empty vector-infected cells. Binding of [(125)I]MRS2500 to P2Y(1) receptors was saturable with a Kd of 1.2nM. Known agonists and antagonists of the P2Y(1) receptor inhibited [(125)I]MRS2500 binding to P2Y(1) receptor-expressing membranes with potencies in agreement with those previously observed in functional assays of this receptor. A high-affinity binding site for [(125)I]MRS2500 also was observed on intact human platelets (Kd=0.61nM) and mouse platelets (Kd=1.20nM) that exhibited the pharmacological selectivity of the P2Y(1) receptor. The densities of sites observed were 151 sites/platelet and 229 sites/platelet in human and mouse platelets, respectively. In contrast, specific binding was not observed in platelets isolated from P2Y(1) receptor(-/-) mice. Taken together, these data illustrate the synthesis and characterization of a novel P2Y(1) receptor radioligand and its utility for examining P2Y(1) receptors natively expressed on human and mouse platelets.
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