Effect of loxiglumide on gallbladder contractile response to cerulein and food in humans

Alberto Malesci, Cristina de Fazio, Susanna Festorazzi, Claudio Bonato, Angela Valentini, Milena Tacconi, Lucio Rovati, Ivo Setnikar

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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 languageEnglish
Pages (from-to)1307-1310
Number of pages4
JournalGastroenterology
Volume98
Issue number5 PART 1
DOIs
Publication statusPublished - 1990

Fingerprint

Ceruletide
Gallbladder Emptying
Gallbladder
Food
Cholecystokinin
Meals
Cholecystokinin Receptors
Intravenous Infusions
Ultrasonography
loxiglumide

ASJC Scopus subject areas

  • Gastroenterology

Cite this

Malesci, A., de Fazio, C., Festorazzi, S., Bonato, C., Valentini, A., Tacconi, M., ... Setnikar, I. (1990). Effect of loxiglumide on gallbladder contractile response to cerulein and food in humans. Gastroenterology, 98(5 PART 1), 1307-1310. https://doi.org/10.1016/0016-5085(90)90349-6

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 journalArticle

Malesci, A, de Fazio, C, Festorazzi, S, Bonato, C, Valentini, A, Tacconi, M, Rovati, L & Setnikar, I 1990, 'Effect of loxiglumide on gallbladder contractile response to cerulein and food in humans', Gastroenterology, vol. 98, no. 5 PART 1, pp. 1307-1310. https://doi.org/10.1016/0016-5085(90)90349-6
Malesci, Alberto ; de Fazio, Cristina ; Festorazzi, Susanna ; Bonato, Claudio ; Valentini, Angela ; Tacconi, Milena ; Rovati, Lucio ; Setnikar, Ivo. / Effect of loxiglumide on gallbladder contractile response to cerulein and food in humans. In: Gastroenterology. 1990 ; Vol. 98, No. 5 PART 1. pp. 1307-1310.
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