Quantification of recombinant and platelet P2Y 1 receptors utilizing a [ 125I]-labeled high-affinity antagonist 2-iodo-N 6-methyl-(N)-methanocarba-2'-deoxyadenosine-3′,5′-bisphosphate ([ 125I]MRS2500)

Pharmacological Research

Volumn 62, Issue 4, 2010, Pages 344-351

  Ohlmann, Philippe ^a   de Castro, Sonia ^b   Brown, Garth G ^c   Gachet, Christian ^a   Jacobson, Kenneth A ^b   Harden, T Kendall ^d  

^a UNIVERSITÉ DE STRASBOURG   (France)

^b NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES   (United States)

^c PERKINELMER INC   (United States)

^d UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

Author keywords

Competitive antagonist; MRS2500; P2Y1 receptor; Platelet; Radioligand

Indexed keywords

(1'2',4'5') PHOSPHORIC ACID DI TERT BUTYL ESTER 1 (DI TERT BUTOXY PHOSPHORYLOXYMETHYL) 4 (6 CHLORO 2 IODINE 125 IODO 9H PURINE YL) BICYCLO [3.1.0]HEX 2 YL ESTER; (1'2',4'5') PHOSPHORIC ACID DI TERT BUTYL ESTER 1 (DI TERT BUTOXY PHOSPHORYLOXYMETHYL) 4 (6 CHLORO 2 TRINETHYLSTANNYLPURIN 9 YL) BICYCLO [3.1.0]HEX 2 YL ESTER; 2' DEOXY 6 N METHYLADENOSINE 3',5' BISPHOSPHATE; 4 (2 IODO 6 METHYLAMINO 9H PURIN 9 YL) 2 PHOSPHONOOXYBICYCLO[3.1.0]HEXANE 1 METHANOL; IODINE 125; PURINERGIC P2Y1 RECEPTOR; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING ASSAY; CONTROLLED STUDY; DRUG BINDING SITE; DRUG PROTEIN BINDING; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; THROMBOCYTE;

ANIMALS; BLOOD PLATELETS; CELL LINE; DEOXYADENINE NUCLEOTIDES; HUMANS; IODINE RADIOISOTOPES; MICE; PROTEIN BINDING; PURINERGIC P2Y RECEPTOR ANTAGONISTS; RADIOPHARMACEUTICALS; RECEPTORS, PURINERGIC P2Y1; RECOMBINANT PROTEINS;

EID: 77955271870     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2010.05.007     Document Type: Article

References (27)

1. Burnstock G. Physiology and pathophysiology of purinergic neurotransmission. Physiol Rev 2007, 87:659-797.
2. Abbracchio M.P., Burnstock G., Boeynaems J.M., Barnard E.A., Boyer J.L., Kennedy C., et al. International Union of Pharmacology LVIII: update on the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy. Pharmacol Rev 2006, 58:281-341.
3. Gachet C. Regulation of platelet functions by P2 receptors. Annu Rev Pharmacol Toxicol 2006, 46:277-300.
4. 1 receptor. Mol Pharmacol 1996, 50:1323-1329.
5. 1 receptor is necessary for adenosine 5'-diphosphate-induced platelet aggregation. Blood 1998, 92:152-159.
6. 1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets. J Biol Chem 1998, 273:2030-2034.
7. 1 receptor. Comb Chem High Throughput Screen 2008, 11:410-419.
8. 1 receptor antagonists. J Med Chem 2003, 46:4974-4987.
9. 1 receptor of human platelets. J Thromb Haemost 2006, 4:861-868.
10. 13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther 2004, 311:1038-1043.
11. 1 and P2cyc receptors. Thromb Haemost 2000, 84:484-491.
12. Baurand A., Eckly A., Hechler B., Kauffenstein G., Galzi J.L., Cazenave J.P., et al. Differential regulation and relocalization of the platelet P2Y receptors after activation: a way to avoid loss of hemostatic properties? Mol Pharmacol. Mol Pharmacol 2005, 67:721-733.
13. Li Q., Chen B.L., Ozdemir V., Ji W., Mao Y.M., Wang L.C., et al. Frequency of genetic polymorphisms of COX1, GPIIIa and P2Y1 in a Chinese population and association with attenuated response to aspirin. Pharmacogenomics 2007, 8:577-586.
14. Fontana P., Remones V., Reny J.L., Aiach M., Gaussem P. P2Y1 gene polymorphism and ADP-induced platelet response. J Thromb Haemost 2005, 3:2349-2350.
15. 1 ADP receptor gene is associated with increased platelet activation response to ADP. Arterioscler Thromb Vasc Biol 2005, 25:252-257.
16. 1 and GP IIIa and response to aspirin and clopidogrel. Thromb Res 2007, 119:355-360.
17. Sibbing D., von Beckerath O., Schomig A., Kastrati A., von Beckerath N. P2Y1 gene A1622G dimorphism is not associated with adenosine diphosphate-induced platelet activation and aggregation after administration of a single high dose of clopidogrel. J Thromb Haemost 2006, 4:912-914.
18. 1 receptors. Br J Pharmacol 2006, 147:459-467.
19. Kung M.P., Kung H.F. Peracetic acid as a superior oxidant for preparation of [iodine-123]IBZM: a potential dopamine D-2 receptor imaging agent. J Lab Compds Radiopharm 1989, 27:691-700.
20. 125I]-CNS 1261): a potential SPECT agent for imaging NMDA receptor activation. Nucl Med Biol 2000, 27:557-564.
21. 1 receptor. Biochem Pharmacol 2004, 68:1995-2002.
22. Cazenave J.P., Ohlmann P., Cassel D., Eckly A., Hechler B., Gachet C. Preparation of washed platelet suspensions from human and rodent blood. Methods Mol Biol 2004, 272:13-28.
23. 1 receptor with a high affinity radiolabeled antagonist. Mol Pharmacol 2002, 62:1249-1257.
24. Baranowska-Lortylewicz J., Helseth L.D., Lai J., Schneiderman M.H., Schneiderman G.S., Dalrymole G.V. Radiolabeling kit/generator for 5-radiohalogenated uridines. J Lab Compd Radiopharm 1994, 34:513-521.
25. 1 receptor. Mol Pharmacol 2004, 65:426-436.
26. 6-methyl 2'-deoxyadenosine 3',5'-bisphosphate. Br J Pharmacol 1998, 124:1-3.
27. 1 receptor antagonist. Eur J Pharmacol 2001, 412:213-221.