Effect of naloxone-3-glucuronide and N-methylnaloxone on the motility of the isolated rat colon after morphine

Reber, Peter; Brenneisen, Rudolf; Flogerzi, Beatrice; Batista, Catarina; Netzer, Peter; Scheurer, Ulrich (2007). Effect of naloxone-3-glucuronide and N-methylnaloxone on the motility of the isolated rat colon after morphine. Digestive diseases and sciences, 52(2), pp. 502-7. New York, N.Y.: Springer 10.1007/s10620-006-9563-9

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The effect of the opioid antagonists naloxone-3-glucuronide and N-methylnaloxone on rat colon motility after morphine stimulation was measured. The rat model consisted of the isolated, vascularly perfused colon. The antagonists (10(-4) M, intraluminally) and morphine (10(-4) M, intra-arterially) were administered from 20 to 30 and from 10 to 50 min, respectively. Colon motility was determined by the luminal outflow. The antagonist concentrations in the luminal and venous outflow were measured by high-performance liquid chromatography. Naloxone-3-glucuronide and N-methylnaloxone reversed the morphine-induced reduction of the luminal outflow to baseline within 10 and 20 min, respectively. These antagonists were then excreted in the luminal outflow and could not be found in the venous samples. Naloxone, produced by hydrolysis or demethylation, was not detectable. In conclusion, highly polar naloxone derivatives peripherally antagonize the motility-lowering effect of morphine in the perfused isolated rat colon, are stable, and are not able to cross the colon-mucosal blood barrier.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > BioMedical Research (DBMR) > DBMR Forschung Mu35 > Forschungsgruppe Phytopharmakologie, Bioanalytik & Pharmakokinetik [discontinued]
04 Faculty of Medicine > Pre-clinic Human Medicine > BioMedical Research (DBMR) > DBMR Forschung Mu35 > Forschungsgruppe Phytopharmakologie, Bioanalytik & Pharmakokinetik [discontinued]

UniBE Contributor:

Brenneisen, Rudolf Max

ISSN:

0163-2116

ISBN:

17211696

Publisher:

Springer

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 14:52

Last Modified:

02 Sep 2020 08:40

Publisher DOI:

10.1007/s10620-006-9563-9

PubMed ID:

17211696

Web of Science ID:

000243904600031

BORIS DOI:

10.7892/boris.21938

URI:

https://boris.unibe.ch/id/eprint/21938 (FactScience: 19652)

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