The gene product is a glycosylated transmembrane protein that functions in both the peripheral and central nervous system to modulate the release of various neurotransmitters.

[7] The receptor is located in the alimentary tract, urinary bladder, heart and adrenal gland as well as the central nervous system (CNS).

[10] Several drugs that act as 5-HT4 selective agonists have recently been introduced into use in both scientific research and clinical medicine.

Some drugs that act as 5-HT4 agonists are also active as 5-HT3 antagonists, such as mosapride, metoclopramide, renzapride, and zacopride, and so these compounds cannot be considered highly selective.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.