​Mechanism of Action

Naronapride is an orally bioavailable, small organic molecule. It was designed to be a potent and selective serotonin 5-HT4 receptor agonist and D2 antagonist. Stimulating 5-HT4 receptors in the gut wall promotes the release of acetylcholine, which works to increase motility of the GI tract, inhibiting D2 receptors removes the brakes on motility of the gut. The high 5-HT4 receptor selectivity minimizes the potential for off-target pharmacological effects. Indeed, it has been shown in animals and in humans to be safe and devoid of adverse cardiovascular effects. Combined 5-HT4 receptor stimulation with D2 receptor inhibition has been proven to be the most effective treatment for motility disorders.