liu.seSearch for publications in DiVA
Change search
ReferencesLink to record
Permanent link

Direct link
A novel tachykinin NK2 receptor antagonist prevents motility-stimulating effects of neurokinin A in small intestine
Linköping University, Faculty of Health Sciences. Linköping University, Department of Biomedicine and Surgery, Clinical Chemistry. Östergötlands Läns Landsting, Centre for Laboratory Medicine, Department of Clinical Chemistry.
Show others and affiliations
2001 (English)In: British Journal of Pharmacology, ISSN 0007-1188, Vol. 134, no 1, 215-223 p.Article in journal (Refereed) Published
Abstract [en]

1. MEN 11420 (nepadutant) is a potent, selective and competitive antagonist of tachykinin NK2 receptors. 2. The objective of the present study was to assess the capability of the drug to antagonize the stimulatory effects of neurokinin A (NKA) on gastrointestinal motility, as well as to change the fasting migrating motor complex (MMC). 3. Thirty-four male volunteers were randomized to treatment with either placebo or MEN 11420 in a double-blinded manner. Effects of MEN 11420 (8 mg intravenously) were evaluated as changes in phases I, II and III of MMC, as well as contraction frequency, amplitude and motility index during baseline conditions and during stimulation of motility using NKA (25 pmol kg-1 min-1 intravenously). 4. NKA preceded by placebo increased the fraction of time occupied by phase II, increased contraction frequency, amplitude and motility index. 5. MEN 11420 effectively antagonized the motility-stimulating effects of NKA. MEN 11420 reduced the phase II-stimulating effect of NKA. In addition, the stimulatory effect of NKA on contraction frequency and amplitude, as well as motility index were inhibited by MEN 11420. MEN 11420 did not affect the characteristics of MMC during saline infusion. 6. Plasma levels of MEN 11420 peaked during the first hour after infusion and decreased to less than half during the first 2 h. 7. In conclusion, intravenous MEN 11420 effectively inhibited NKA-stimulated, but not basal gastrointestinal motility, and was well tolerated by all subjects.

Place, publisher, year, edition, pages
2001. Vol. 134, no 1, 215-223 p.
National Category
Medical and Health Sciences
URN: urn:nbn:se:liu:diva-25427Local ID: 9873OAI: diva2:245756
Available from: 2009-10-07 Created: 2009-10-07 Last updated: 2011-01-13

Open Access in DiVA

No full text

Search in DiVA

By author/editor
Theodorsson, Elvar
By organisation
Faculty of Health SciencesClinical ChemistryDepartment of Clinical Chemistry
In the same journal
British Journal of Pharmacology
Medical and Health Sciences

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Total: 93 hits
ReferencesLink to record
Permanent link

Direct link