Multiple gastrointestinal-relevant receptors

The term 'Multiple gastrointestinal-relevant receptors' refers to a heterogeneous collection of proteins, primarily G protein-coupled receptors (GPCRs), ion channels, and enzymes, that regulate the physiological functions of the digestive tract. These targets include opioid receptors (mu, delta, and kappa), serotonin receptors (specifically 5-HT3 and 5-HT4), cholecystokinin receptors, and guanylate cyclase-C, which collectively coordinate gut motility, mucosal secretion, and the transmission of pain signals from the gut to the brain (PubMed: 29329707). These receptors are central to the pathophysiology of functional gastrointestinal disorders (FGIDs) such as irritable bowel syndrome (IBS) and chronic idiopathic constipation (CIC). Pharmacological agents targeting these receptors often aim for a multi-modal approach; for instance, eluxadoline acts on three different opioid receptors to manage diarrhea and pain while minimizing side effects (FDA Label: Eluxadoline). Understanding the interplay between these multiple receptors is crucial for developing therapies that can normalize bowel function without causing systemic adverse effects or significant disruption to the enteric nervous system (PubMed: 24311436).

Other names

GI receptorsGastrointestinal receptorsEnteric receptorsGut-brain axis receptors

Modulation of enteric nervous system signaling and intestinal epithelial transport through the simultaneous or sequential activation/inhibition of diverse pathways including cAMP/cGMP production and calcium signaling (PubMed: 27144306).