Synthesis of prostacyclin and thromboxane A2 by rat gastric mucosa. Comparison of 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido (1,1-a)-pyrimidine-3-carboxamide and cimetidine.
The production of prostacyclin (PGI2) and thromboxane A2 (TXA2) was studied in an indometacin-induced ulcer model in rats. The specific activities of prostacyclin synthetase and thromboxane synthetase as well as the tissue content of these prostaglandins were determined. The anti-ulcer effect of cimetidine and a novel agent, i.e. 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido(1,1-a)-pyrimidine-3- carboxamide (Chinoin-127) was compared in this respect. The indometacin treatment shifted the balance of TXA2/PGI2 to the formation of TXA2, and the anti-ulcer agents repaired it. The role of this balance in cytoprotection is discussed.
Rózsa
I
I
Department of Pharmacological Research, Chinoin Pharmaceutical and Chemical Works, Budapest, Hungary.
Kapui
Z
Z
Szécsi
T
T
Hermecz
I
I
Blaskó
G
G
D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology; D002927:Cimetidine / Q000494:pharmacology*; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System; D011464:Epoprostenol / Q000096:biosynthesis*; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism*; D007213:Indomethacin / Q000494:pharmacology; D019746:Intramolecular Oxidoreductases; D007535:Isomerases / Q000037:antagonists & inhibitors; D008297:Male; D011744:Pyrimidinones / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013928:Thromboxane A2 / Q000096:biosynthesis*; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors
D000897:Anti-Ulcer Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D011744:Pyrimidinones; C020954:chinoin 127; D013928:Thromboxane A2; D002927:Cimetidine; D003577:Cytochrome P-450 Enzyme System; D011464:Epoprostenol; D007535:Isomerases; D019746:Intramolecular Oxidoreductases; C022461:prostacyclin synthetase; D013930:Thromboxane-A Synthase; D007213:Indomethacin