The synthesis of N-acetyl-leukotriene E4 and its effects on cardiovascular and respiratory function of the anesthetized pig.
The effects of the putative biliary metabolite of the peptido-leukotrienes, N-acetyl-leukotriene (LT) E4 has been investigated in the anesthetized pig. Intravenous bolus doses of synthetic N-acetyl-LTE4 produced minimal respiratory and cardiovascular actions in the pig. N-acetyl-LTE4 was approximately 100-fold less active than LTC4. The actions of N-acetyl-LTE4 were not blocked by pretreatment of the animals with indomethacin (5 mg/kg iv) or with a selective LTD4 antagonist L-649,923 (5 mg/kg plus 2 mg/kg/hr iv). In summary, N-acetyl-LTE4 exerts weak actions in the pig which is consistent with the acetylation process being a mechanism of detoxification.
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002302:Cardiac Output / Q000187:drug effects; D002319:Cardiovascular System / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005260:Female; D007213:Indomethacin / Q000494:pharmacology; D007275:Injections, Intravenous; D017999:Leukotriene E4 / Q000031:analogs & derivatives*; D008297:Male; D010654:Phenylbutyrates / Q000494:pharmacology; D012137:Respiratory System / Q000187:drug effects*; D013189:SRS-A / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D013552:Swine
D010654:Phenylbutyrates; D013189:SRS-A; D017999:Leukotriene E4; C047630:N-acetylleukotriene E4; C050033:L 649923; D007213:Indomethacin