Insights into the central pathways involved in the emetic and behavioural responses to exendin-4 in the ferret

Auton Neurosci. 2017 Jan:202:122-135. doi: 10.1016/j.autneu.2016.09.003. Epub 2016 Sep 14.

Abstract

Background: GLP-1 receptor agonists are utilised for the treatment of Type-2 diabetes but can be associated with undesirable effects of nausea and vomiting.

Objectives: To investigate the role of GLP-1 receptors in mechanisms of emesis, behaviours indicative of nausea (BIN) and food intake in the ferret.

Results: Exendin-4 (10 and 30nmol, i.c.v.) induced emesis, inhibited food intake, and increased the frequency of BIN. Increases in c-Fos in the brainstem, midbrain and forebrain occurred in animals exhibiting emesis; no activation of the brainstem occurred in animals not vomiting. Exendin-4 (10nmol, i.c.v.) when preceded by i.c.v. saline (15μl), was not emetic but induced BIN and inhibited food intake; exendin (9-39) (100nmol) reduced BIN only. c-Fos showed that consistent with the absence of emesis in saline/exendin-4 treated animals there was no increase in c-Fos in the brainstem, but it increased in midbrain and forebrain nuclei. Excepting the amygdala, exendin (9-39) was without efffect on the increases in c-Fos. Analysis of c-Fos data showed a positive linear relationship between midbrain and forebrain areas irrespective of the occurrence of emesis induced by exendin-4. In contrast, brainstem and midbrain c-Fos levels were positively correlated, but only in animals with emesis.

Conclusions: The brainstem is critical for exendin-4-induced emesis but suppression of food intake and BIN involves more rostral brain sites. Exendin-4-induced BIN and c-Fos activation of the amygdala are sensitive to exendin (9-39), whereas the suppression of food intake is not implicating separate control mechanisms for emesis and BIN.

Keywords: Emesis; Exendin-4, exendin (9–39); Ferret; Glucagon-like peptide-1; Glucagon-like peptide-1 receptor; Nausea; c-Fos.

MeSH terms

  • Animals
  • Brain / drug effects*
  • Brain / metabolism
  • Brain / pathology
  • Catheters, Indwelling
  • Dose-Response Relationship, Drug
  • Eating / drug effects
  • Eating / physiology
  • Emetics / pharmacology*
  • Exenatide
  • Ferrets
  • Glucagon-Like Peptide 1 / agonists
  • Glucagon-Like Peptide 1 / metabolism
  • Immunohistochemistry
  • Injections, Intraventricular
  • Male
  • Motor Activity / drug effects
  • Motor Activity / physiology
  • Nausea / chemically induced*
  • Nausea / metabolism
  • Nausea / pathology
  • Neural Pathways / drug effects
  • Neural Pathways / metabolism
  • Neural Pathways / pathology
  • Peptides / pharmacology*
  • Proto-Oncogene Proteins c-fos / metabolism
  • Venoms / pharmacology*
  • Vomiting / chemically induced*
  • Vomiting / metabolism
  • Vomiting / pathology

Substances

  • Emetics
  • Peptides
  • Proto-Oncogene Proteins c-fos
  • Venoms
  • Glucagon-Like Peptide 1
  • Exenatide