The novel suramin analogue NF864 selectively blocks P2X1 receptors in human platelets with potency in the low nanomolar range

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 372, Issue 1, 2005, Pages 1-13

  Horner, Susanne ^a   Menke, Kirsten ^a   Hildebrandt, Caren ^a   Kassack, Matthias U ^b   Nickel, Peter ^b   Ullmann, Heiko ^b   Mahaut Smith, Martyn P ^c   Lambrecht, Günter ^a  

^a GOETHE UNIVERSITY   (Germany)

^b UNIVERSITY OF BONN   (Germany)

^c UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

Ca2+ i; Aggregation; NF449; NF864; P2X1; P2Y1; Platelet P2 receptors; Shape change

Indexed keywords

4,4',4'',4''' [CARBONYLBIS[IMINO 5,1,3 BENZENETRIYLBIS(CARBONYLIMINO)]] TETRAKISBENZENE 1,3 DISULFONIC ACID OCTASODIUM; 4,4',4'',4''' [CARBONYLBIS[IMINO 5,1,3 BENZENETRIYLBIS(CARBONYLIMINO)]] TETRAKISBENZENESULFONIC ACID TETRASODIUM; 8,8' [CARBONYLBIS(IMINO 1,3 PHENYLENECARBONYLIMINO)]BIS(NAPHTHALENE 1,3,5 TRISULFONIC ACID)HEXASODIUM; 8,8' [CARBONYLBIS(IMINO 1,3 PHENYLENECARBONYLIMINO)]BISBENZENE 1,3 DISULFONIC ACID TETRASODIUM; 8,8',8'',8''' [CARBONYLBIS[IMINO 5,1,3 BENZENETRIYLBIS(CARBONYLIMINO)]] TETRAKISNAPHTHALENE 1,3,5 TRISULFONIC ACID DODECASODIUM; ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; CARBONYL DERIVATIVE; NF 023; NF 110; NF 449; NF 864; PURINE P2X1 RECEPTOR; PURINE P2Y1 RECEPTOR; PURINE P2Y12 RECEPTOR; RECEPTOR BLOCKING AGENT; SURAMIN; UNCLASSIFIED DRUG;

ARTICLE; CALCIUM CELL LEVEL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; FLUORESCENCE; HUMAN; HUMAN CELL; NORMAL HUMAN; RECEPTOR BLOCKING; THROMBOCYTE; THROMBOCYTE AGGREGATION; THROMBOCYTE SHAPE; TURBIDIMETRY;

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; APYRASE; BLOOD PLATELETS; CALCIUM; CELL SHAPE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; LEAST-SQUARES ANALYSIS; LINEAR MODELS; PHENYLMERCURY COMPOUNDS; PLATELET AGGREGATION INHIBITORS; RECEPTORS, PURINERGIC P2; SURAMIN; THIONUCLEOTIDES;

EID: 26244468128     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-005-1085-z     Document Type: Article

References (64)

1. 14 receptor) adds diversity to the P2Y receptor family. Trends Pharmacol Sci 24:52-55
2. 1 receptor antagonist. Eur J Pharmacol 412:213-221
3. 6-methyl 2′-deoxyadenosine 3′,5′-bisphosphate. Br J Pharmacol 124:1-3
4. 1 receptors. Naunyn-Schmiedebergs Arch Pharmacol 364:285-290
5. Burnstock G (2004) Introduction: P2 receptors. Curr Top Med Chem 4:793-803
6. 50. A closer look at the Cheng-Prussoff equation, the Schild plot and related power equations. J Pharmacol Toxicol Methods 46:61-71
7. i) and the concentration of inhibitor which causes 50 per cent inhibition (150) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108
8. 12 receptor in thrombosis. Curr Opin Hematol 10:333-338
9. Cusack NJ, Hourani SMO (1982) Specific but noncompetitive inhibition by 2-alkylthio analogues of adenosine 5′-monophosphate and adenosine 5′-triphosphate fo human platelet aggregation induced by adenosine 5′-diphosphate. Br J Pharmacol 75:397-400
10. 12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270. Blood 101:3908-3914
11. 1 receptors. J Thromb Haemost 1:2626-2635
12. 1-deficient mice. Nat Med 5:1199-1202
13. Fiske CH, Subbarow Y (1925) The colorimetric determination of phosphorus. J Biol Chem 66:375-400
14. Frolenkov GI, Belyantseva IA, Kurc M, Mastroianni MA, Kachar B (1998) Cochlear outer hair cell electromotility can provide force for both low and high intensity distortion product otoacoustic emissions. Hear Res 126:67-74
15. Gachet C (2001) ADP receptors of platelets and their inhibition. Thromb Haemost 86:222-232
16. 2+ indicators with greatly improved fluorescence properties. J Biol Chem 260:3440-3450
17. 3 receptor-selective antagonist. Naunyn-Schmiedebergs Arch Pharmacol 369(Suppl 1):R28
18. 1 receptor is necessary for adenosine 3′,5-diphosphate-induced platelet aggregation. Blood 92:152-159
19. 1 cation channel in thrombosis of small arteries in vivo. J Exp Med 198:661-667
20. Hechler B, Magnenat S, Zighetti ML, Kassack MU, Ullmann H, Cazenave JP, Evans R, Cattaneo M, Gachet C (2005) Inhibition of platelet functions and thrombosis through selective or non selective inhibition of the platelet P2 receptors with increasing doses of NF449. J Pharmacol Exp Ther 314:232-243
21. Hollopeter G, Jantzen HM, Vincent D, Li G, England L, Ramakrishnan V, Yang RB, Nurden P, Nurden A, Julius D, Conley PB (2001) Identification of the platelet ADP receptor targeted by antithrombotic drugs. Nature 409:202-207
22. 1-selective in whole tissues? Drug Dev Res 56:A153
23. Horner S, Hildebrandt C, Menke K, Lambrecht G (2004a) Pharmacological properties of the homomeric bivalent ligand CLII and its monomer, MRS2159, at native P2 receptor subtypes. Naunyn-Schmiedebergs Arch Pharmacol 369 (Suppl 1):R30
24. 1 receptors in human platelets with nanomolar potency. Purines 2004, Chapel Hill, NC, USA, Abstract Book: 74W
25. Hourani, SMO (2001) Discovery and recognition of purine receptor subtypes on platelets. Drug Dev Res 52:140-149
26. Hourani SM, Hall DA, Nieman CJ (1992) Effects of the P2-purinoceptor antagonist, suramin, on human platelet aggregation induced by adenosine 5′-diphosphate. Br J Pharmacol 105:453-457
27. Jacobson KA, Jarvis MF, Williams M (2002) Purine and pyrimidine P2 receptors as drug targets. J Med Chem 45:4057-4093
28. Jacobson KA, Costanzi S, Olino M, Joshi BV, Besada P, Xu B, Tchilibon S (2004) Molecular recognition at purine and pyrimidine nucleotide (P2) receptors. Curr Top Med Chem 4:805-819
29. Jantzen HM, Gousset L, Bhaskar V, Vincent D, Tai A, Reynolds EE, Conley PB (1999) Evidence for two distinct G-protein-coupled ADP receptors mediating platelet activation. Thromb Haemost 81:111-117
30. 1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets. J Biol Chem 273:2030-2034
31. 1 receptor antagonist. Eur J Med Chem 39:345-357
32. 3 integrin-a phosphoinositide 3-kinase-dependent mechanism. FEBS Lett 505:281-290
33. Kettlun AM, Leyton M, Valenzuela MA, Mancilla M, Traverso-Cori A (1992) Identification and subcellular localization of two isoenzymes of apyrase from solanum tuberosum. Phytochemistry 31:1889-1894
34. Khakh BS, Burnstock G, Kennedy C, King BF, North RA, Ségué la P, Voigt M, Humphrey PPA (2001) International Union of Pharmacology. XXIV. Current status of the nomenclature and properties of P2X receptors and their subunits. Pharmacol Rev 53:107-118
35. 1 receptors. J Med Chem 44:340-349
36. 13 results in shape change and Rho/Rho-kinase-mediated myosin light chain phosphorylation in mouse platelets. J Cell Biol 144:745-754
37. 2+ channels in PC12 cells by antithrombotic drugs. Br J Pharmacol 138:343-350
38. Kunapuli SP, Ding Z, Dorsam RT, Kim S, Murugappan S, Quinton TM (2003) ADP receptors-targets for developing antithrombotic agents. Curr Pharm Des 9:2303-2316
39. Lambrecht G (2000) Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications. Naunyn-Schmiedebergs Arch Pharmacol 362:340-350
40. Lambrecht G, Braun K, Damer S, Ganso M, Hildebrandt C, Ullmann H, Kassack MU, Nickel P (2002) Structure-activity relationships of suramin and pyridoxal-5′-phosphate derivatives as P2 receptor antagonists. Curr Pharm Des 8:2371-2399
41. 1 receptor is an ADP receptor antagonized by ATP and expressed in platelets and megakaryoblastic cells. FEBS Lett 403:26-30
42. 1 receptor-null mice. J Clin Invest 104:1731-1737
43. 1 receptors in platelet activation. Platelets 15:131-144
44. 1 receptors in human platelets. Naunyn-Schmiedebergs Arch Pharmacol 367(Suppl 1):R35
45. Michal F, Maguire MH, Gough G (1969) 2-Methylthioadenosine-5′- phosphate: a specific inhibitor of platelet aggregation. Nature 222:1073-1074
46. Mills DC (1996) ADP receptors on platelets. Thromb Haemost 76:835-856
47. 1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. J Med Chem 41:1456-1466
48. Müller W, Wollert U (1976) Spectroscopic studies on the complex formation of suramin with bovine and human serum albumin. Biochem Biophys Acta 427:465-480
49. North RA (2002) Molecular physiology of P2X receptors. Physiol Rev 82:1013-1067
50. q. Blood 96:2134-2139
51. 1 ion channel acts as a positive regulator of platelet responses to collagen. Thromb Haemost 86:1264-1271
52. 1 ion channel in transgenic mice generates a novel prothombotic phenotype. Blood 101:3969-3976
53. Paul BZ, Daniel JL, Kunapuli SP (1999) Platelet shape change is mediated by both calcium- dependent and -independent signaling pathways. Role of p160 Rho-associated coiled-coil-containing protein kinase in platelet shape change. J Biol Chem 274:28293-28300
54. Paul BZ, Kim S, Dangelmaier C, Nagaswami C, Jin J, Hartwig JH, Weisel JW, Daniel JL, Kunapuli SP (2003) Dynamic regulation of microtubule coils in ADP-induced platelet shape change by p160ROCK (Rho-kinase). Platelets 14:159-169
55. 1 receptor antagonist. Neuropharmacology 48:461-468
56. 2+ influx on functional responses in human platelets. Thromb Haemost 88:495-502
57. 1 purinoceptors with α,β-methylene ATP. Thromb Haemost 85:303-308
58. 12 receptor-mediated platelet functional responses. Blood 104:1335-1343
59. Soto F, Lambrecht G, Nickel P, Stühmer W, Busch AE (1999) Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors. Neuropharmacology 38:141-149
60. 12 ADP-receptor. J Thromb Haemost 2:135-146
61. 1 receptor. Mol Pharmacol 60:432-439
62. Tallarida RJ, Murray RB (1986) Manual of pharmacologic calculations with computer programs. Springer, Berlin Heidelberg New York
63. Von Kügelgen I, Wetter A (2000) Molecular pharmacology of P2Y receptors. Naunyn-Schmiedebergs Arch Pharmacol 362:310-323
64. Wilde JI, Retzer M, Siess W, Watson SP (2000) ADP-induced platelet shape change: an investigation of the signalling pathways involved and their dependence on the method of platelet preparation. Platelets 11:286-295