LACK OF EFFECT OF THE SPECIFIC CHOLECYSTOKININ RECEPTOR ANTAGONIST LOXIGLUMIDE ON CHOLECYSTOKININ CLEARANCE FROM PLASMA IN MAN

Saline or loxiglumide (2.5 mg kg‐1 in 10 min, followed by 5 mg kg‐1 h‐1 for 200 min) was administered intravenously in random order to six healthy subjects. After 60 min cholecystokinin (CCK‐33) was infused (0.5 i.d.u. kg‐1 h‐1 for 1 h then 1.0 i.d.u. kg‐1 h‐1 for 1 h). Loxiglumide did not change basal levels of CCK and did not augment plasma CCK‐immunoreactivity during CCK‐33 infusion. After cessation of the CCK‐infusion, plasma CCK concentrations decreased rapidly to basal values within 12 min, and the elimination half‐life during loxiglumide infusion (4.8 +/− 0.8 min) was not significantly different from that during saline infusion (4.2 +/− 1.0 min). These results suggest that loxiglumide does not interfere with the distribution and metabolism of CCK. 1990 The British Pharmacological Society