Title : Biochemical and pharmacological profiles of loxiglumide, a novel cholecystokinin-A receptor antagonist.

Pub. Date : 1998 Jan

PMID : 9522034






6 Functional Relationships(s)
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1 Radioligand displacement assay was performed to characterize the selectivity of loxiglumide to CCK-A (cholecystokinin-A) receptor (rat pancreas and bovine gallbladder) and CCK-B/gastrin receptors (guinea pig cerebral cortex and guinea pig gastric parietal cell). loxiglumide cholecystokinin Cavia porcellus
2 Loxiglumide inhibited 125I-CCK-8 binding to rat pancreatic and bovine gallbladder membranes with IC50 values of 195 and 77.1 nmol/l, respectively. loxiglumide cholecystokinin Cavia porcellus
3 Loxiglumide also inhibited 125I-CCK-8 binding to guinea pig cerebral cortex membranes and parietal cells with IC50 values of 12363 and 15455 nmol/l, respectively. loxiglumide cholecystokinin Cavia porcellus
4 These results indicate that the affinity of loxiglumide to CCK-A receptor is at least 63 times greater than that to CCK-B/gastrin receptors. loxiglumide cholecystokinin Cavia porcellus
5 In vitro functional studies utilizing CCK-induced contractions of the isolated guinea pig gallbladder and ileum further demonstrate that loxiglumide acts as a competitive CCK antagonist with a high affinity to these tissues (gallbladder, pA2:6.71). loxiglumide cholecystokinin Cavia porcellus
6 In vitro functional studies utilizing CCK-induced contractions of the isolated guinea pig gallbladder and ileum further demonstrate that loxiglumide acts as a competitive CCK antagonist with a high affinity to these tissues (gallbladder, pA2:6.71). loxiglumide cholecystokinin Cavia porcellus