Abstract
The present study investigated the effect of loxiglumide, a new selective cholecystokinin-receptor antagonist, on the gallbladder contractile responses to caerulein and to food in humans. In 6 healthy men, the gallbladder emptying driven by intravenous infusion of stepwise increasing doses of cerulein (10-80 ng/kg · h) and that induced by a 550-cal standard meal were monitored by ultrasonography. In both sets of experiments, the effect of loxiglumide was tested at various infusional rates against a control infusion of saline. An infusional rate of 2.5 mg/kg · h of loxiglumide abolished the gallbladder response even to maximal doses of cerulein, whereas a rate of 1.0 mg/kg · h counteracted the cholecystokinetic activity of cerulein up to the dose of 20 ng/kg · h. In postprandial experiments, the cholecystokinin antagonist dose-dependently inhibited the physiologic gallbladder contraction. The maximal gallbladder emptying, which always occurred 85 min after the meal, was 71.1% ± 3.3% of basal volume in control studies, 39.2% ± 1.8% during infusion of 2.5 mg/kg · h of loxiglumide, and 17.3% ± 5.9% when 5.0 mg/kg · h were infused. A dose of 7.5 mg/kg · h of loxiglumide was able to prevent any postprandial emptying of the gallbladder. The present study shows that a selective cholecystokinin receptorial blockade competitively antagonizes cerulein-induced gallbladder contraction and dose-dependently inhibits postprandial gallbladder emptying.
| Original language | English |
|---|---|
| Pages (from-to) | 1307-1310 |
| Number of pages | 4 |
| Journal | Gastroenterology |
| Volume | 98 |
| Issue number | 5 PART 1 |
| DOIs | |
| Publication status | Published - 1990 |
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- Gastroenterology
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Effect of loxiglumide on gallbladder contractile response to cerulein and food in humans. / Malesci, Alberto; de Fazio, Cristina; Festorazzi, Susanna; Bonato, Claudio; Valentini, Angela; Tacconi, Milena; Rovati, Lucio; Setnikar, Ivo.
In: Gastroenterology, Vol. 98, No. 5 PART 1, 1990, p. 1307-1310.Research output: Contribution to journal › Article
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TY - JOUR
T1 - Effect of loxiglumide on gallbladder contractile response to cerulein and food in humans
AU - Malesci, Alberto
AU - de Fazio, Cristina
AU - Festorazzi, Susanna
AU - Bonato, Claudio
AU - Valentini, Angela
AU - Tacconi, Milena
AU - Rovati, Lucio
AU - Setnikar, Ivo
PY - 1990
Y1 - 1990
N2 - The present study investigated the effect of loxiglumide, a new selective cholecystokinin-receptor antagonist, on the gallbladder contractile responses to caerulein and to food in humans. In 6 healthy men, the gallbladder emptying driven by intravenous infusion of stepwise increasing doses of cerulein (10-80 ng/kg · h) and that induced by a 550-cal standard meal were monitored by ultrasonography. In both sets of experiments, the effect of loxiglumide was tested at various infusional rates against a control infusion of saline. An infusional rate of 2.5 mg/kg · h of loxiglumide abolished the gallbladder response even to maximal doses of cerulein, whereas a rate of 1.0 mg/kg · h counteracted the cholecystokinetic activity of cerulein up to the dose of 20 ng/kg · h. In postprandial experiments, the cholecystokinin antagonist dose-dependently inhibited the physiologic gallbladder contraction. The maximal gallbladder emptying, which always occurred 85 min after the meal, was 71.1% ± 3.3% of basal volume in control studies, 39.2% ± 1.8% during infusion of 2.5 mg/kg · h of loxiglumide, and 17.3% ± 5.9% when 5.0 mg/kg · h were infused. A dose of 7.5 mg/kg · h of loxiglumide was able to prevent any postprandial emptying of the gallbladder. The present study shows that a selective cholecystokinin receptorial blockade competitively antagonizes cerulein-induced gallbladder contraction and dose-dependently inhibits postprandial gallbladder emptying.
AB - The present study investigated the effect of loxiglumide, a new selective cholecystokinin-receptor antagonist, on the gallbladder contractile responses to caerulein and to food in humans. In 6 healthy men, the gallbladder emptying driven by intravenous infusion of stepwise increasing doses of cerulein (10-80 ng/kg · h) and that induced by a 550-cal standard meal were monitored by ultrasonography. In both sets of experiments, the effect of loxiglumide was tested at various infusional rates against a control infusion of saline. An infusional rate of 2.5 mg/kg · h of loxiglumide abolished the gallbladder response even to maximal doses of cerulein, whereas a rate of 1.0 mg/kg · h counteracted the cholecystokinetic activity of cerulein up to the dose of 20 ng/kg · h. In postprandial experiments, the cholecystokinin antagonist dose-dependently inhibited the physiologic gallbladder contraction. The maximal gallbladder emptying, which always occurred 85 min after the meal, was 71.1% ± 3.3% of basal volume in control studies, 39.2% ± 1.8% during infusion of 2.5 mg/kg · h of loxiglumide, and 17.3% ± 5.9% when 5.0 mg/kg · h were infused. A dose of 7.5 mg/kg · h of loxiglumide was able to prevent any postprandial emptying of the gallbladder. The present study shows that a selective cholecystokinin receptorial blockade competitively antagonizes cerulein-induced gallbladder contraction and dose-dependently inhibits postprandial gallbladder emptying.
UR - http://www.scopus.com/inward/record.url?scp=0025322128&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0025322128&partnerID=8YFLogxK
U2 - 10.1016/0016-5085(90)90349-6
DO - 10.1016/0016-5085(90)90349-6
M3 - Article
C2 - 2323521
AN - SCOPUS:0025322128
VL - 98
SP - 1307
EP - 1310
JO - Gastroenterology
JF - Gastroenterology
SN - 0016-5085
IS - 5 PART 1
ER -