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PROSTAGLANDIN ANTAGONISM BY SODIUM p ‐BENZYL‐4‐[1‐OXO‐2‐(4‐CHLOROBENZYL)‐3‐PHENYLPROPYL]PHENYL PHOSPHONATE (N‐O164)
Author(s) -
EAKINS K.E.,
RAJADHYAKSHA V.,
SCHROER R.
Publication year - 1976
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1976.tb07709.x
Subject(s) - chemistry , antagonist , prostaglandin antagonist , pharmacology , prostaglandin , medicine , endocrinology , biochemistry , biology , receptor
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 E 2 and F 2α 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 E 2 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.