Antivasoconstrictor and antiaggregatory activities of picotamide unrelated to thromboxane A2 antagonism

Thrombosis and Haemostasis

Volumn 78, Issue 5, 1997, Pages 1385-1391

  Vezza, Roberta ^a   Spina, Domenico ^b   Tallarida, Ronald J ^c   Nathan, Malevika ^a   Page, Clive P ^b   Gresele, Paolo ^a  

^a UNIVERSITY OF PERUGIA   (Italy)

^b KING'S COLLEGE LONDON   (United Kingdom)

^c TEMPLE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

15 HYDROXY 11ALPHA,9ALPHA EPOXYMETHANOPROSTA 5,13 DIENOIC ACID; PHENYLEPHRINE; PICOTAMIDE; POTASSIUM ION; RIDOGREL; SEROTONIN; SEROTONIN 2 RECEPTOR; SULOTROBAN; THROMBOXANE A2; THROMBOXANE RECEPTOR BLOCKING AGENT; THROMBOXANE SYNTHASE; VASOACTIVE AGENT;

ANIMAL CELL; ANIMAL TISSUE; AORTA; ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; MALE; NONHUMAN; PRIORITY JOURNAL; RABBIT; THROMBOCYTE AGGREGATION INHIBITION; THROMBOCYTE SHAPE; VASCULAR SMOOTH MUSCLE; VASODILATATION;

EID: 0030727255     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0038-1665416     Document Type: Article

References (46)

1. 2. Pharmacol Rev 1979; 30: 293-331.
2. 2 as an amplifying signal for other agonists. Am J Cardiol 1991; 68: 11B-5B.
3. 2. Science 1976; 193: 461-70.
4. 2 receptors. J Lipid Mediators Cell Signalling 1995; 12: 361-78.
5. 2 receptor subtypes. A radioligand binding study of human platelets. J Clin Invest 1989; 84: 1883-91.
6. 2 receptors. Am J Physiol 1991; 260: H327-34.
7. 2 analogue (U46619) on human platelets by means of human granulocytic elastase and chymotrypsin. Biochem Pharmacol 1989; 38: 3213-7.
8. 2 analogues in human platelets. Discrimination of two binding sites linked to distinct effector systems. J Biol Chem 1990; 265: 6836-44.
9. 2 receptors. Am J Physiol 1991; 261: R145-53.
10. 2 receptors: distinct subtypes mediate vascular smooth muscle contraction and platelet aggregation. J Pharmacol Exp Ther 1991; 258: 74-81.
11. 2 stimulated signal transduction in vascular smooth muscle. J Pharmacol Exp Ther 1993; 265: 447-56.
12. Gresele P, Deckmyn H, Nenci GG, Vermylen J. Thromboxane synthase inhibitors, thromboxane receptor antagonists and dual blockers in thrombotic disorders. Trends Pharmacol Sci 1991; 12: 158-63.
13. 2 synthase inhibition alone and in combination: comparison of anti-aggregatory efficacy in human platelets. Br J Pharmacol 1991; 102: 497-505.
14. Salvati P, Dho L, Ukmar G, Vorga L, Rimoldi O, Patrono C. A comparative evaluation of thromboxane receptor blockade, thromboxane synthase inhibition and both in animal models of arterial thrombosis. J Pharmacol Exp Ther 1994; 269: 238-45.
15. 2 receptors. Evidence for difference subclasses in the rat. Biochem Pharmacol 1991; 42: 537-44.
16. Gresele P, Deckmyn H, Arnout J, Nenci GG, Vermylen J. Characterization of N N', bis (3-picolyl)-4 -methoxy -isophtalamide (picotamide) as a dual thromboxane synthase inhibitor/thromboxane receptor antagonist in human platelets. Thomb Haemost 1989; 61: 479-84.
17. 2 receptor antagonist. Br J Pharmacol 1994; 112: 81-6.
18. Gresele P, Corona C, Alberti P, Nenci GG. Picotamide protects mice from death in a pulmonary embolism model by a mechanism independent from thromboxane suppression. Thromb Haemost 1990; 64: 80-6.
19. Janssens WJ, Deckmyn H, Gresele P, Vermylen J. BM13.177 selectively inhibits endoperoxide analogue induced vascular contractions. Arch Int Pharmacodyn Ther 1985; 276: 28-34.
20. Spina D, Harrison S, Page CP. Regulation by phosphodiesterase isoenzymes of non-adrenergic non-cholinergic contraction in guinea pig isolated main bronchus. Br J Pharmacol 1995; 116: 2334-40.
21. 3 potentiates platelet aggregation by priming protein kinase C. Blood 1993; 73: 2006-13.
22. 2-receptor antagonist. Agents Action 1982; 12: 388-97.
23. Arunlakshana O, Schild HO. Some quantitative uses of drug antagonists. Br J Pharmacol 1959; 14: 48-58.
24. Tallarida RJ, Murray RB. Manual of pharmacologic calculation with computer programs, 2nd ed. Springer-Verlag, New York, 1987.
25. Chou TC. Derivation and properties of Michaelis-Menten type and Hill type equations for reference ligands. J Theor Biol 1976; 39: 253-76.
26. Armstrong RA, Jones RL, Peesapati V, Will SG, Wilson NH. Competitive antagonism at thromboxane receptors in human platelets. Br J Pharmacol 1985; 84: 595-607.
27. Keith RA, Solama AI. Individual variation of prostanoid agonist responses in rabbit aorta: evidence for the independent regulation of prostanoid receptor subtypes. Br J Pharmacol 1987; 92: 133-48.
28. Fernandez del Pozo B, Perez-Vizcaino F, Villamore E, Zaragoza F, Tamargo J. Stereoselective effects of the enantiomers, quinidine and quinine, on depolarization-and agonist-mediated responses in rat isolated aorta. Br J Pharmacol 1996; 117: 105-10.
29. 2-mimetic, the actions of which are slowly reversed by receptor blockade. Br J Pharmacol 1989; 96: 875-87.
30. Jones RL, Peesapati V, Wilson NH. Antagonism of the thromboxane sensitive contractile system of the rabbit aorta, dog saphenous vein and guinea pig trachea. Br J Pharmacol 1982; 76: 423-38.
31. Patscheke H, Stegmeier K, Muller-Beckman B, Sponer G, Staiger C, Neugebauer G. Inhibitory effect of selective thromboxane receptor antagonist BM13.177 on platelet aggregation, vasoconstriction and sudden death. Biomed Biochim Acta 1984; 43: 5312-8.
32. 2/prostaglandin endoperoxide receptor antagonist. J Cardiovasc Pharmacol 1993; 21: 441-7.
33. 2 receptor binding by picotamide. Eur J Pharmacol 1989; 169: 85-93.
34. Janssens WJ, Cools FJS, Hoskens LAM, Nueten JM. Effect of ridogrel on vascular contractions caused by vasoactive substances released during platelet activation. Thromb Haemost 1990; 64: 91-6.
35. Robertson RM, Robertson D. Drugs used for the treatment of myocardial ischemia, In: The Pharmacological Basis of Therapeutics. Hardman LE, Limbird LE, Molinoff PB, Ruddon RW, Gilman AG, eds. McGraw Hill, New York, NY 1996, pp 759-79.
36. Fossati T, Parisi S, Abbiati G, Castiglioni C. Determination of picotamide in human plasma and urine by high performance liquid chromatography. J Chromatogr 1992; 577: 382-6.
37. 2 receptor antagonist. Evidence for the existence of an uptake system. Eicosanoids 1990; 3: 139-43.
38. Feniunk W, Humprey PPA, Perren MJ, Watts AD. A comparison of 5-hydroxytryptamine receptors mediating contraction in rabbit aorta and dog saphenous vein: evidence for different receptor types obtained by use of selective agonists and antagonists. Br J Pharmacol 1985; 86: 697-704.
39. Gresele P, Vezza R, Nenci GG. Inhibition of cytoplasmic calcium movements in stimulated platelets by picotamide. Thromb Haemost 1989; 62: A552.
40. Pulcinelli FM, Pignatelli P, Riondino S, Parisi S, Castiglioni C, Gazzaniga P. Effect of picotamide on the calcium mobilization and phospholipase C activation in human platelets. Thromb Res 1994; 74: 453-61.
41. +-contracted rabbit and rat aortae. J Physiol 1988; 400: 395-404.
42. Christie MI, Lewis MJ. Vascular smooth muscle sensitivity to endothelium-derived relaxing factor is different in different arteries. Br J Pharmacol 1988, 95: 630-6.
43. Feldhoff CM, Gresele P, Pieters G, Vermylen J. Acetylsalicylic acid, BM13.177 and picotamide improve the survival of endotoxin-infused rabbit. Thromb Res 1988; 52: 487-92.
44. Balsano F, Violi F. Effect of picotamide on the clinical progression of peripheral vascular disease. A double blind placebo-controlled study. The ADEP group. Circulation 1993; 87: 1563-9.
45. 2 in ischaemic heart disease. Blood Coag Fibrinol 1990; 1: 201-20.
46. 2 inhibitor: importance of activated monocytes. Coron Artery Dis 1994; 5: 137-45.