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Studies of three non‐peptide cholecystokinin antagonists (devazepide, lorglumide and loxiglumide) in human isolated alimentary muscle and guinea‐pig ileum
Author(s) -
D'Amato M.,
Stamford I.F.,
Bennett A.
Publication year - 1991
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.1476-5381.1991.tb12184.x
Subject(s) - cholecystokinin , medicine , endocrinology , proglumide , cholecystokinin receptor , antagonist , biology , ileum , receptor
1 Three recently described non‐peptide cholecystokinin (CCK) antagonists (devazepide, lorglumide, loxiglumide) have been studied for their antagonism of the contraction to cholecystokinin‐octapeptide (CCK‐OP) in human alimentary muscle and guinea‐pig intestine. 2 Each antagonist caused a concentration‐dependent inhibition of the contraction induced by CCK‐OP, regardless of regional and species differences. 3 The potencies of each drug, estimated by use of an adaptation of the Cheng & Prusoff equation, were similar in the different regions of human alimentary tract (weighted mean apparent pK B , ± s.e.mean: devazepide, 5.76 ± 0.08, n = 20; lorglumide, 5.82 ± 0.04, n = 25; loxiglumide, 5.87 ± 0.07, n = 24). 4 In contrast, the potencies differed markedly in the guinea‐pig ileum. Apparent pK B values obtained by the same method as with human tissues were, mean ± s.e.mean: devazepide, 10.61 ± 0.61; lorglumide, 7.43 ± 0.20; loxiglumide, 6.67 ±0.12. pK B values obtained from classical competition experiments were: devazepide, 10.09 ± 0.09; lorglumide 7.70 ± 0.12; loxiglumide 6.08 ± 0.22. 5 The CCK receptors in human gut muscle from different regions seem to be similar, but there appear to be species differences.