SCH-50971


SCH-50971 is a histamine H3 receptor agonist which was under development for the treatment of anxiety disorders, gastrointestinal disorders, and migraine but was never marketed.

Pharmacology

The drug acts as a potent, selective, and high-affinity agonist of the histamine H3 receptor. It has negligible affinity for the histamine H1 receptor and other assessed receptors. The drug is also not a histamine H2 receptor antagonist. It has greatly improved selectivity compared to the earlier selective histamine H3 receptor agonist (R)-α-methylhistamine. The drug is orally active and shows anti-allergy effects, antimigraine effects, sedative and hypnotic effects, and hypolocomotion in animals. In terms of chemical structure, it is a cyclized pyrrolidine derivative of histamine.

Development

SCH-50971 was under development by Schering-Plough. It reached the discovery or preclinical research stage of development. The development of the drug was discontinued by 2001. SCH-50971 was first described in the scientific literature by 1994.