scholarly journals The Potent Inhibition of Vapiprost, a Novel Thromboxane A2 Receptor Antagonist, on the Secondary Aggregation and ATP Release of Human Platelets.

1997 ◽  
Vol 20 (6) ◽  
pp. 625-631 ◽  
Author(s):  
Shuichi HORIE ◽  
Mayumi YAMADA ◽  
Megumi SATOH ◽  
Shinobu NORITAKE ◽  
Sayuri HIRAISHI ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Atp Release ◽  
Thromboxane A2 ◽  
Human Platelets ◽  
Thromboxane A2 Receptor ◽  
Potent Inhibition

scholarly journals Intrinsic activity of the non-prostanoid thromboxane A2 receptor antagonist, daltroban (BM 13,505), in human platelets in vitro and in the rat vasculature in vivo

1995 ◽  
Vol 115 (1) ◽  
pp. 210-216 ◽  
Author(s):  
Frédéric Bertolino ◽  
Jean-Pierre Valentin ◽  
Myriam Maffre ◽  
Françoise Grelac ◽  
Anne-Marie Bessac ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Thromboxane A2 ◽  
Human Platelets ◽  
Intrinsic Activity ◽  
Thromboxane A2 Receptor

scholarly journals Thromboxane-induced phosphatidate formation in human platelets. Relationship to receptor occupancy and to changes in cytosolic free calcium

1984 ◽  
Vol 219 (3) ◽  
pp. 833-842 ◽  
Author(s):  
W K Pollock ◽  
R A Armstrong ◽  
L J Brydon ◽  
R L Jones ◽  
D E MacIntyre
Keyword(s):  
Receptor Antagonist ◽  
Platelet Activation ◽  
Human Platelet ◽  
Thromboxane A2 ◽  
Receptor Occupancy ◽  
Phospholipid Metabolism ◽  
Human Platelets ◽  
Thromboxane A2 Receptor ◽  
Agonist Concentration ◽  
Inositol Phospholipid

The inter-relationships between receptor occupancy, inositol phospholipid metabolism and elevation of cytosolic free Ca2+ in thromboxane A2-induced human platelet activation were investigated by using the stable thromboxane A2 mimetic, 9,11-epoxymethanoprostaglandin H2, and the thromboxane A2 receptor antagonist, EPO45. 9,11-Epoxymethanoprostaglandin H2 stimulated platelet phosphatidylinositol metabolism as indicated by the rapid accumulation of [32P]phosphatidate and later accumulation of [32P]phosphatidylinositol in platelets pre-labelled with [32P]Pi. These effects of 9,11-epoxymethanoprostaglandin H2 were concentration-dependent and half-maximal [32P]phosphatidate formation occurred at an agonist concentration of 54 +/- 8 nM. With platelets labelled with the fluorescent Ca2+ indicator quin 2, resting cytosolic free Ca2+ was 86 +/- 12 nM. 9,11-Epoxymethanoprostaglandin H2 induced a rapid, concentration-dependent elevation of cytosolic free Ca2+ to a maximum of 300-700 nM. Half-maximal stimulation was observed at an agonist concentration of 80 +/- 23 nM. The thromboxane A2 receptor antagonist EPO45 selectively inhibited 9,11-epoxymethanoprostaglandin H2-induced [32P]phosphatidate formation and elevation of cytosolic free Ca2+, indicating that both events are sequelae of receptor occupancy. Human platelets contain a single class of stereospecific, saturable, high affinity (KD = 70 +/- 13 nM) binding sites for 9,11-epoxymethano[3H]prostaglandin H2. The concentration-response curve for receptor occupancy (9,11-epoxymethano-[3H]prostaglandin H2 binding) is similar to that for 9,11-epoxymethanoprostaglandin H2-induced [32P]phosphatidate formation and for elevation of cytosolic free Ca2+. These observations indicate that human platelet thromboxane A2 receptor occupation is closely linked to inositol phospholipid metabolism and to elevation of cytosolic free Ca2+. Both such events may be necessary for thromboxane A2-induced human platelet activation.

Carrier-Mediated Active Transport of a Novel Thromboxane A2 Receptor Antagonist [2-(4-Chlorophenylsulfonylaminomethyl)indan-5-yl]acetate (Z-335) into Rat Liver

2002 ◽  
Vol 30 (5) ◽  
pp. 498-504 ◽  
Author(s):  
Yoshihiro Kawabata ◽  
Shigeru Furuta ◽  
Yutaka Shinozaki ◽  
Tadashi Kurimoto ◽  
Ryuichiro Nishigaki
Keyword(s):  
Receptor Antagonist ◽  
Active Transport ◽  
Rat Liver ◽  
Thromboxane A2 ◽  
Thromboxane A2 Receptor
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