Gastrointestinal motility-related targets

Gastrointestinal motility-related targets represent a diverse set of receptors and enzymes that regulate the mechanical movement of the digestive system (NIH, 2024). These targets are primarily located within the enteric nervous system, on smooth muscle cells, and on interstitial cells of Cajal, where they coordinate peristalsis and gastric emptying (StatPearls, 2023). Key therapeutic targets include the 5-HT4 serotonin receptor, the motilin receptor, the ghrelin receptor, and the dopamine D2 receptor (Nature Reviews Gastroenterology & Hepatology, 2016). Drugs that act on these targets, collectively known as prokinetics, are used to manage conditions such as gastroparesis, chronic constipation, and gastroesophageal reflux disease (GERD) (Cleveland Clinic, 2024). For example, 5-HT4 agonists like prucalopride enhance colonic transit, while D2 antagonists like metoclopramide promote gastric emptying and provide antiemetic effects (Frontiers in Pharmacology, 2021). However, the clinical use of many agents in this class is constrained by significant safety concerns, including neurological side effects for dopamine antagonists and potential cardiotoxicity for certain serotonergic drugs (NIH, 2024).

Other names

Prokinetic targetsGI motility receptorsGastrointestinal prokinetic targetsGastrointestinal motility-related receptors

Modulation of gastrointestinal transit through agonism of 5-HT4, motilin, or ghrelin receptors, antagonism of dopamine D2 or mu-opioid receptors, or inhibition of acetylcholinesterase (Frontiers in Pharmacology, 2021; NIH, 2024).