Pharmacological actions of S-145, a novel thromboxane A2 antagonist, in various smooth muscles
نویسندگان
چکیده
منابع مشابه
Effect of a novel thromboxane A2 receptor antagonist, S-1452, on postischemic brain injury in rats.
BACKGROUND AND PURPOSE Arachidonate metabolites have been implicated in the development of cerebral injury after ischemia. Particular importance has been placed on the balance of thromboxane A2 and prostaglandin I2 because of its regulative activity on platelet functions and arterial tone. The purpose of the present study was to shed light on the role of thromboxane A2 in postischemic brain inj...
متن کاملIdentification of rat and human cytochrome P450 forms involved in the metabolism of the thromboxane A2 receptor antagonist (+)-S-145.
(+)-S-145 [5-(+)-(Z)-7-[(1R, 2S, 3S, 4S)-3-phenylsulfonylaminobicyclo[2.2.1]hept-2-yl]-heptenoic acid] and its beta-oxidized metabolites [two [bisnor or dihydro (DH)-bisnor] or four (tetranor) carbon-shortened products at the carboxyl side chain] are hydroxylated at the C-5 or C-6 position of the bicyclo ring by microsomal monooxygenases. We investigated the oxidative metabolism of (+)-S-145 an...
متن کاملThromboxane A2 Synthase Inhibitor and Thromboxane A2/Prostaglandin Endoperoxide Receptor Antagonist, Versus Aspirin
Background Aspirin, by nonselectively blocking cyclooxygenase both in platelets and in endothelial cells, not only inhibits the thromboxane A2 pathway of platelet activation but at the same time also the generation of vasodilating and platelet-inhibitory prostanoids, such as prostacyclin, by the endothelial cells. Ridogrel, by inhibiting thromboxane A2 synthase and blocking the thromboxane A2/p...
متن کاملIdentification of Rat and Human Cytochrome P450 Forms Involved in the Metabolism of the Thromboxane A2 Receptor Antagonist (1)-s-145
(1)-S-145 {5-(1)-(Z)-7-[(1R, 2S, 3S, 4S)-3-phenylsulfonylaminobicyclo[2.2.1]hept-2-yl]-heptenoic acid} and its b-oxidized metabolites {two [bisnor or dihydro (DH)-bisnor] or four (tetranor) carbon-shortened products at the carboxyl side chain} are hydroxylated at the C-5 or C-6 position of the bicyclo ring by microsomal monooxygenases. We investigated the oxidative metabolism of (1)-S-145 and i...
متن کاملCerebral arterial smooth muscle contraction by thromboxane A2.
The contractile effects of thromboxane A2 (TxA2), a labile arachidonic acid metabolite, were studied in arterial smooth muscle strips. TxA2 was generated upon the addition of 255 nM prostaglandin cyclic endoperoxide H2 to human platelet particles in the muscle bath. Using the isometric contaction produced by 40 mM K+ in isotonic saline as the reference contraction, bovine middle cerebral artery...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1988
ISSN: 0021-5198
DOI: 10.1016/s0021-5198(19)57681-8