Dose-response effects of oral loxiglumide on postprandial gall-bladder emptying in man

A. Malesci, C. De Fazio, S. Festorazzi, C. Bonato, A. Valentini, M. Tacconi, M. Bekkering, G. Giacovelli, M. D'Amato, L. C. Rovati

Research output: Contribution to journalArticle

Abstract

The effect of two different single oral doses of loxiglumide (CR 1505, CAS 107097-80-3) on gall-bladder emptying induced by a 550-cal standard mixed meal in 6 healthy volunteers was studied. Following placebo, the maximal gall-bladder emptying occurred about 90 min after the meal (minimal residual gall-bladder volume 27.4% of basal volume). Loxiglumide 400 or 800 mg dose-dependently inhibited the physiological gall-bladder emptying. Loxiglumide plasma levels dose-dependently increased. The inhibition of gall-bladder emptying and the kinetic of loxiglumide plasma levels were temporally related. The results of the present study confirm that oral loxiglumide is a potent orally active cholecystokinin (CCK) antagonist in man and that CCK is the major physiological mediator of gallbladder emptying in response to meal.

Original languageEnglish
Pages (from-to)1359-1362
Number of pages4
JournalArzneimittel-Forschung/Drug Research
Volume42
Issue number11
Publication statusPublished - 1992

Keywords

  • CAS 107097-80-3
  • cholecystokinin antagonist
  • CR 1505
  • Loxiglumide, clinical studies

ASJC Scopus subject areas

  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

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    Malesci, A., De Fazio, C., Festorazzi, S., Bonato, C., Valentini, A., Tacconi, M., Bekkering, M., Giacovelli, G., D'Amato, M., & Rovati, L. C. (1992). Dose-response effects of oral loxiglumide on postprandial gall-bladder emptying in man. Arzneimittel-Forschung/Drug Research, 42(11), 1359-1362.