P2Y1-receptors in human platelets which are pharmacologically distinct from P2Y(ADP)-receptors

British Journal of Pharmacology

Volumn 124, Issue 1, 1998, Pages 157-164

  Fagura, M S ^a   Dainty, I A ^a   McKay, G D ^a   Kirk, I P ^a   Humphries, R G ^a   Robertson, M J ^a   Dougall, I G ^a   Leff, P ^a  

^a Astra Charnwood ^*  (United Kingdom)

Author keywords

Adenosine 3' phosphate 5' phosphate; ADP; AR C66096; ATP; Human washed platelets; Intracellular calcium measurements; Jurkat cells; P2Y1 receptors; Receptor reserve

Indexed keywords

ADENINE NUCLEOTIDE DERIVATIVE; ADENOSINE 3' PHOSPHATE 5' PHOSPHOSULFATE; ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; AR C 66096; CALCIUM ION; PURINE P2Y RECEPTOR; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG; 2 PROPYLTHIO D BETA,GAMMA DIFLUOROMETHYLENE ATP; 2-PROPYLTHIO-D-BETA,GAMMA-DIFLUOROMETHYLENE ATP; ADENOSINE 3' PHOSPHATE 5' PHOSPHATE; ADENOSINE 3'-PHOSPHATE-5'-PHOSPHATE; ANTITHROMBOCYTIC AGENT; CALCIUM; DRUG DERIVATIVE; PURINE P2 RECEPTOR; PURINE P2Y1 RECEPTOR; RECOMBINANT PROTEIN;

ARTICLE; CALCIUM CELL LEVEL; CELL TYPE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; HUMAN; HUMAN CELL; LEUKEMIA CELL LINE; PRIORITY JOURNAL; RECEPTOR DENSITY; THROMBOCYTE; ANIMAL; CATTLE; DRUG EFFECT; FEMALE; GENETIC TRANSFECTION; MALE; METABOLISM;

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; ANIMALS; BLOOD PLATELETS; CALCIUM; CATTLE; FEMALE; HUMANS; JURKAT CELLS; MALE; PLATELET AGGREGATION INHIBITORS; RECEPTORS, PURINERGIC P2; RECOMBINANT PROTEINS; TRANSFECTION;

EID: 0031596463     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0701827     Document Type: Article

References (37)

1. BLACK, J.W. & LEFF, P. (1983). Operational models of pharmacological agonism. Proc. R. Soc. B., 220, 141 162.
2. BLACK, J.W., LEFF, P., SHANKLEY, N.P. & WOOD, J. (1985). An operational model of agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol, 84, 561 571.
3. BOYER, J.L., O'TUEL, J.W., FISCHER, B. JACOBSEN, K.A. & HARDEN, T.K. (1995). Potent agonist action of 2-thioether derivatives of adenine nucleotides at adenylyl cyclase-linked P2Y-receptors. Br. J. Pharmacol., 116, 2611 2616.
4. 1-receptor. Mol. Pharmacol., 50, 1323 1329.
5. BURNSTOCK, G. & KING, B.F. (1996). Numbering of cloned P2 receptors. Drug Dev. Res., 38, 67 71.
6. CATTANEO, M., LECCHI, A., RANDI, A.M., MCGREGOR, J.L. & MANNUCI, P.M. (1992). Identification of a new congenital detect of platelet function characterized by severe impairment of platelet responses to adenosine diphosphate. Blood, 80, 2787 2796.
7. CONLEY, P., VINCENT, D., TAI, A., BHASKAR, V., LI, G., CHIU, E., KARTIK, A. & JANTZEN, H.M. (1996). Cloning of two receptors from a human megakaryocytic cell line. Drug Dev. Res., 37, 111.
8. CUSACK, N.J. & HOURANI, S.M.O. (1982). Adenosine 5′-diphosphate antagonists and human platelets: no evidence that aggregation and inhibition of stimulated adenylate cyclase are mediated by different receptors. Br. J. Pharmacol., 76, 221 227.
9. CUSACK, N.J. & PETTEY, C.J. (1996). Effects of phosphate-modified analogs of adenosine 5′-diphosphate and adenosine 5′-triphosphate at P2T-receptors mediating human platelet activation by ADP. Drug Dev. Res., 37, 212 - 222.
10. 1-purinoceptor transfected into Jurkat cells. Br. J. Pharmacol., 120, 299P.
11. FEOLDE, E., VIGNE, P. BREITTMAYER, J.P. & FRELIN, C (1995). ATP. a partial agonist of atypical P2Y receptors in rat brain microvascular endothelial cells. Br. J. Pharmacol., 115, 1199 1203.
12. FILTZ, T.M., LI, Q., BOYER, J.L., NICHOLAS, R.A. & HARDEN, T.K. (1994). Expression of a cloned P2Y purinergic receptor that couples to phospholipase C. Mol. Pharmacol., 46, 8 - 14.
13. FREDHOLM, B.B., ABBRACCHIO, M.P. BURNSTOCK, G., DUBYAK, G.R., HARDEN, T.K., JACOBSON, K.A., SCHWABE, U. & WILLIAMS, M. (1997). Towards a revised nomenclature for P1 and P2 receptors. Trends Pharmacol. Sci., 18, 79 82.
14. GABBERTA, J., YANG, X., KOWALSKA, M.A., SUN, L. & DHANASEKARAN, N. (1997). Platelet signal transduction defect with Gα subunit dysfunction and diminished Gaq in a patient with abnormal platelet responses. Proc. Natl. Acad. Sci. U.S.A., 94, 8750 - 8755.
15. GACHET, C., CATTANEO, M., OHLMANN, P., HECHLER, B., LECCHL, A., CHEVALIER, J., CASSEL, D., MANNUCCIO, P.M. & CAZENAVE, J.P. (1995). Receptors on blood platelets: further pharmacological and clinical evidence to suggest the presence of two ADP receptors. Br. J. Haematol., 91, 434 444.
16. 1. Biochem. Pharmacol., 40, 2683 2687.
17. GACHET, C., HECHLER, B., LEON, C., VTAL, C., LERAY, C., OHLMANN, P. & CAZENAVE, J. (1997). Activation of ADP receptors and platelet function. Thromb. Haemost., 78, 271 275.
18. GEAR, A.R.L. (1993). Platelet adhesion, shape change and aggregation: rapid initiation and signal transduction events. Can. J. Physiol. Pharmacol., 72, 285 - 294.
19. HALL, D.A. & HOURANI, S.M.O. (1993). Effects of analogues of adenine nucleotides on increase in intracellular calcium mediated by P2T-receptors on human blood platelets. Br. J. Pharmacol., 108, 728 733.
20. HENDERSON, D.J., ELLIOT, D.G., SMITH, G.M., WEBB, T.E. & DAINTY, I.A. (1995). Cloning and characterisation of a bovine P2Y receptor. Biochim. Biophys. Res. Commun., 212, 648 656.
21. HOURANI, S.M.O. & CUSACK, N.J. (1991). Pharmacological receptors on blood platelets. Pharmacol. Rev., 43, 243 298.
22. HOURANI, S.M.O. & HALL, D.A. (1994). Receptors for ADP on human blood platelets. Trends Pharmacol. Sci., 15, 103 - 108.
23. HUMPHRIES, R.G., TOMLINSON, W., INGALL, A.H., CAGE, P.A. & LEFF, P. (1994). FPL 66096LT: a novel, highly potent and selective antagonist at human platelet P2T-receptors. Br. J. Pharmacol., 113, 1057 1063.
24. LEEF, P., PRENTICE, D.J., GILES, H., MARTIN, G.R. & WOOD, J. (1990). Estimation of agonist affinity and efficacy by direct, operational model-fitting. J. Pharmacol. Methods, 23, 225 237.
25. 1 receptor is an ADP receptor antagonised by ATP and expressed in platelets and megakaryoblastic cells. FEBS Lett., 403, 26 30.
26. 1 not P2T receptors in human platelets. J. Biol. Chem., 271, 2879 2881.
27. MURGO, A.J., CONTRERA, J.G. & SISTARE, F.D. (1994). Evidence for separate calcium-signaling P2T and P2U receptors in human megakaryocytic Dami cells. Blood, 83, 1258 1267.
28. MURGO, A.J. & SISTARE, F.D. (1992). K562 leukemia cells express P2T (adenosine di-phosphate) purinergic receptors. J. Pharmacol. Exp. Ther., 261, 580 - 585.
29. NICHOLAS, R.A., WATT, W.C., LAZAROWSKI, E.R., LI, Q & HARDEN, T.K. (1996). Uridine nucleotide selectivity of three phospholipuse C-activating P2-receptors: Identification of a UDP-selective, a UTP-selective and an ATP- and UTP-specific receptor. Mol. Pharmacol., 50, 224 229.
30. OFFERMANNS, S., TOOMBS, C.F., HU, Y. & SIMON, M. (1997). Defective platelet activation in Gαq-deficient mice. Nature, 389, 183 186.
31. SANDERSON, U.M., HEPINSTALL, S., VICKERS, J. & LOSCHE, W. (1996). Studies on the effects of agonists and antagonists on platelet shape change and platelet aggregation in whole blood. Blood Coag. Fibrinol., 7, 245 - 248.
32. SARGEANT, P. & SAGE, S.O. (1994). Calcium signalling in platelets and other nonexcitable cells. Pharmacol. Ther., 64, 395 443.
33. 1 receptor to phospholipase C. Br. J. Pharmacol., 122, 1021 - 1024.
34. SISTARE, F.D., ROSENZWEIG, B.A., CONTRERA, J.G. & JORDAN, B. (1994). Separate P2T and P2U purinergic receptors with similar second messenger signalling pathways in UMR-106 osteoblasts. J. Pharmacol. Exp. Ther., 269, 1049 1061.
35. 2 values and associated analysis. J. Pharmacol. Exp. Ther., 207, 705 718.
36. TOMLINSON, W., HUMPHRIES, R.G., ROBERTSON, M.J. & LEFF, P. (1997). ARL 67085 and ARL 66096 are slowly dissociating competitive P2T-purinoceptor antagonists. Br. J. Pharmacol., 120, 131P.
37. 2-agonism by clonidine and dimaprit in an adenylate cyclase assay. Agents Actions, 16, 222 226.