Elsevier

Life Sciences

Volume 23, Issue 25, 18 December 1978, Pages 2509-2515
Life Sciences

Prostaglandin synthesis inhibited by formamidine pesticides

https://doi.org/10.1016/0024-3205(78)90176-5Get rights and content

Abstract

The formamidine pesticides, chlordimeform and amitraz, were shown to have both antipyretic and anti-inflammatory activity when given intraperitoneally to rats at 5 to 80 mg per kg. They reduced yeast-induced fever in rats with potencies intermediate between those of indomethacin and aspirin, and antagonized the carageenin-induced swelling of the hind paw. In both these actions, chlordimeform was more potent than amitraz. Both formamidines also inhibited the synthesis of prostaglandin E2 from arachidonic acid by bovine seminal vesicle microsomes. At an arachidonic acid concentration of 0.4 μM, the I50 values for chlordimeform and amitraz were 34 and 880 μM respectively, compared to 0.4 μM and 790 μM for indomethacin and aspirin. These aspirin-like actions may provide a clue to some of the physiological effects of the formamidines, which represent a new and unsual group of prostaglandin synthetase inhibitors.

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