SEROTONIN ANTAGONISTS

Abstract

The realisation that serotonin plays a role not only in the carcinoid syndrome but also in migraine, nociception, dumping syndrome, vascular disease and hypertension, has led to an enormous amount of activity in search of serotonin antagonists. Numerous such pharmacological agents have been identified but only few have found their way into clinical use. All of them are competitive serotonin inhibitors, in that they vie for the same receptor as the amine itself and are thus able to block its action as well as imitate its effects. By far the widest use of such inhibitors is in the prevention of migraine, where they have effectively eliminated the dread of an attack from the life of the majority of patients. Whilst useful in the control of diarrhea in patients with carcinoid and dumping syndromes, their role in these diseases is limited. However, the possible role of serotonin in hypertension and nociception opens new avenues in the use of existing serotonin antagonists and calls for the discovery of a new generation of such pharmacological agents for the control of these conditions.