PROSTAGLANDIN ANTAGONISM BY SODIUM p‐BENZYL‐4‐[1‐OXO‐2‐(4‐CHLOROBENZYL)‐3‐PHENYLPROPYL]PHENYL PHOSPHONATE (N‐O164)

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Abstract
1 The ability of sodium p-benzyl-4-[1-oxo-2-(4-chlorobenzyl)-3-phenylpropyl]phenyl phosphonate (N-0164) to antagonize contractions produced by prostaglandins E2 and F2α on isolated preparations of gerbil, rat and guinea-pig gastrointestinal muscle has been studied. 2 N-0164 was found to be a potent, partially selective prostaglandin antagonist in these isolated smooth muscle preparations. The blockade produced by N-0164 in the isolated stomach strip of the rat had some, but not all, the characteristics of a competitive antagonism. 3 N-0164 produced a dose-dependent decrease in tone in the rat stomach strip that was abolished by pretreatment of the preparation with indomethacin. 4 N-0164 prevented diarrhoea induced by prostaglandin E2 in mice when given by intraperitoneal injection but was less effective when given orally. 5 N-0164 inhibited oedema induced with croton-oil and pyridine-ether in the mouse ear. 6 N-0164 delayed the onset of erythema following ultraviolet irradiation of guinea-pig skin only when an equimolar amount of pralidoxime chloride was added to the vehicle. 7 It is concluded that N-0164 is a potent, partially selective prostaglandin antagonist on several isolated smooth muscle preparations. N-0164 exhibits activity in vivo particularly following local application when problems associated with penetration and distribution are minimized.

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