GIPR Agonism Inhibits PYY-Induced Nausea-Like Behavior

Diabetes. 2022 Jul 1;71(7):1410-1423. doi: 10.2337/db21-0848.

Abstract

The induction of nausea and emesis is a major barrier to maximizing the weight loss profile of obesity medications, and therefore, identifying mechanisms that improve tolerability could result in added therapeutic benefit. The development of peptide YY (PYY)-based approaches to treat obesity are no exception, as PYY receptor agonism is often accompanied by nausea and vomiting. Here, we sought to determine whether glucose-dependent insulinotropic polypeptide (GIP) receptor (GIPR) agonism reduces PYY-induced nausea-like behavior in mice. We found that central and peripheral administration of a GIPR agonist reduced conditioned taste avoidance (CTA) without affecting hypophagia mediated by a PYY analog. The receptors for GIP and PYY (Gipr and Npy2r) were found to be expressed by the same neurons in the area postrema (AP), a brainstem nucleus involved in detecting aversive stimuli. Peripheral administration of a GIPR agonist induced neuronal activation (cFos) in the AP. Further, whole-brain cFos analyses indicated that PYY-induced CTA was associated with augmented neuronal activity in the parabrachial nucleus (PBN), a brainstem nucleus that relays aversive/emetic signals to brain regions that control feeding behavior. Importantly, GIPR agonism reduced PYY-mediated neuronal activity in the PBN, providing a potential mechanistic explanation for how GIPR agonist treatment reduces PYY-induced nausea-like behavior. Together, the results of our study indicate a novel mechanism by which GIP-based therapeutics may have benefit in improving the tolerability of weight loss agents.

MeSH terms

  • Animals
  • Anti-Obesity Agents* / adverse effects
  • Mice
  • Nausea / chemically induced
  • Nausea / drug therapy
  • Obesity / drug therapy
  • Peptide YY* / adverse effects
  • Receptors, Gastrointestinal Hormone* / agonists

Substances

  • Anti-Obesity Agents
  • Receptors, Gastrointestinal Hormone
  • Peptide YY

Associated data

  • figshare/10.2337/figshare.19601518