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The differential antiemetic properties of GLP-1 receptor antagonist, exendin (9-39) in Suncus murinus (house musk shrew).

Abstract
The use of glucagon-like peptide-1 (7-36) amide (GLP-1) receptor agonists for the treatment of type 2 diabetes mellitus is commonly associated with nausea and vomiting. Previous studies using Suncus murinus revealed that the GLP-1 receptor agonist, exendin-4, induces emesis via the brainstem and/or hypothalamus. The present study investigated the mechanism of exendin-4-induced emesis in more detail. Ondansetron (1 mg/kg, s.c.) and CP-99,994 (10 mg/kg, s.c) failed to reduce emesis induced by exendin-4 (3 nmol, i.c.v.), suggesting that 5-HT3 and NK1 receptors are not involved in the mechanism. In other studies, the GLP-1 receptor antagonist, exendin (9-39), antagonised emesis and c-Fos expression in the brainstem and the paraventricular hypothalamus induced by the chemotherapeutic drug cisplatin (30 mg/kg, i.p.; p < 0.05), but not the emesis induced by nicotine (5 mg/kg, s.c.; p > 0.05), or copper sulphate pentahydrate (120 mg/kg, p.o.; p > 0.05). GLP-1 receptors may therefore represent a potential target for drugs to prevent chemotherapy-induced emesis in situations where 5-HT3 and NK1 receptor antagonists fail.
AuthorsSze Wa Chan, Zengbing Lu, Ge Lin, David Tai Wai Yew, Chi Kong Yeung, John A Rudd
JournalNeuropharmacology (Neuropharmacology) Vol. 83 Pg. 71-8 (Aug 2014) ISSN: 1873-7064 [Electronic] England
PMID24726308 (Publication Type: Journal Article)
CopyrightCopyright © 2014 Elsevier Ltd. All rights reserved.
Chemical References
  • Antiemetics
  • Glucagon-Like Peptide-1 Receptor
  • Peptide Fragments
  • Peptides
  • Piperidines
  • Proto-Oncogene Proteins c-fos
  • Receptors, Glucagon
  • Venoms
  • 3-(2-methoxybenzylamino)-2-phenylpiperidine
  • Ondansetron
  • exendin (9-39)
  • Exenatide
Topics
  • Animals
  • Antiemetics (pharmacology)
  • Brain (metabolism)
  • Exenatide
  • Glucagon-Like Peptide-1 Receptor
  • Male
  • Ondansetron (pharmacology)
  • Peptide Fragments (pharmacology)
  • Peptides
  • Piperidines (pharmacology)
  • Proto-Oncogene Proteins c-fos (metabolism)
  • Receptors, Glucagon (antagonists & inhibitors)
  • Shrews
  • Venoms
  • Vomiting (chemically induced, metabolism)

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