Role of Thromboxane A2

Ambler, J. E.; Birch, Jill; Maguire, E.D.; Wallis, Robert B.

doi:10.1007/978-1-4615-9442-0_21

Cited by 11 publications

(1 citation statement)

References 24 publications

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“…The thrombus produced subsequent to the injury to the vascular endothelium, is platelet-rich and resembles clinically observed thrombi (Matsuno et al, 1991). TXA2, although relatively labile, is synthesized in large quantities by platelets in response to a variety of stimuli (Best et al, 1980;Ambler et al, 1985). Thromboxane receptor antagonists (TRAs) such as vapiprost (Lumley et al, 1989), sulotoroban (Shebuski et al, 1988;Fujita et al, 1988) and Ah-23848 (Brezinski et al, 1988) have been shown to interfer with platelet function through specific competitive inhibition of the platelet membrane receptor that binds either TXA2 or the cyclic endoperoxides intermediate, PGH2.…”

Section: Discussionmentioning

confidence: 99%

Effects of vapiprost, a novel thromboxane receptor antagonist, on thrombus formation and vascular patency after thrombolysis by tissue‐type plasminogen activator

Matsuno

Umemura

Takiguchi

et al. 1992

British J Pharmacology

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A thrombus was induced in the rat femoral artery by endothelial damage due to the photochemical reaction between systemically‐injected Rose Bengal and transillumination with green light (wavelength: 540 nm). The artery of the control rat was completely occluded in 302.8 ± 27.0 s after the initiation of the reaction. Pretreatment with vapiprost (0.1, 0.3 and 1.0 mg kg−1, i.v., 5 min before the reaction) prolonged the time required to occlude the femoral artery in a dose‐dependent manner. The efficacy of vapiprost on the time required for occlusion was over 10 times higher than that of aspirin which was administered 30 min before the reaction. The thrombolytic effects of tissue‐type plasminogen activator (tPA) on the established arterial thrombus in the presence and absence of vapiprost were also studied in the same model. When vapiprost (0.3 mg kg−1, i.v.) was administered just before tPA infusion (100 μg kg−1 min−1 for 30 min), the time required to reperfuse the occluded artery was reduced, the incidence of the reperfusion was increased and the arterial blood flow after reperfusion was improved. When vapiprost (1.0 mg kg−1 daily p.o.) was administered for 1 week after the establishment of reperfusion by tPA combined with vapiprost, the patency of the reperfused artery was improved and the femoral arterial blood flow was better preserved than after treatment with only tPA. These findings suggest that this thromboxane receptor antagonist may be a useful adjunct to anti‐thrombotic therapy. The combination therapy with tPA may be more effective than treatment with tPA alone and provides greater protection against reocculsion after reperfusion.

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Section: Discussionmentioning

confidence: 99%

Effects of vapiprost, a novel thromboxane receptor antagonist, on thrombus formation and vascular patency after thrombolysis by tissue‐type plasminogen activator

Matsuno

Umemura

Takiguchi

et al. 1992

British J Pharmacology

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5-Substituted pyridylisoxazoles as effective inhibitors of platelet aggregation

et al. 2014

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A series of 5 substituted 3 pyridylisoxazoles were synthesized using [3+2] cycloaddition of nitrile oxides to alkynes with variation of substituents at position 5 of the isoxazole ring without additional synthetic stages and with retention of 2 pyridyl , 3 pyridyl, and 4 pyridyl substitu ents at position 3 of the isoxazole ring. Substituted pyridylisoxazoles are the potential anti aggregatory agents showing in vitro activity in the concentration range from 1•10 -6 mol L -1 to 1•10 -4 mol L -1 toward the human platelet rich blood plasma with arachidonic acid being used as the inductor of aggregation. These compounds do not act as cyclooxygenase or thromboxane synthase inhibitors, nor as thrombin inhibitors.

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