5-HT Receptor

Serotonin (5-hydroxytryptamine, 5-HT) produces its effects through a variety of membrane-bound receptors. 5-HT and its receptors are found both in the central and peripheral nervous system (CNS/PNS), as well as in a number of nonneuronal tissues in the gut, cardiovascular system and blood. In evolutionary terms, 5-HT is one of the oldest neurotransmitters and has been implicated in the aetiology of numerous disease states, including depression, anxiety, social phobia, schizophrenia, and obsessive–compulsive and panic disorders; in addition to migraine, hypertension, pulmonary hypertension, eating disorders, vomiting and, more recently, irritable bowel syndrome (IBS). 
5-HT is probably unique among the monoamines in that its effects are subserved by as many as 13 distinct heptahelical, G-protein-coupled receptors (GPCRs) and one (presumably a family of) ligand-gated ion channel(s). These receptors are divided into seven distinct classes (5-HT1 to 5-HT7) largely on the basis of their structural and operational characteristics.Not surprisingly, the 5-HT receptor family has been a long-standing target of intense research, in both the academia and the pharmaceutical industry, even before the complexity of the system was unravelled by molecular cloning.


1.Hoyer D, et al. Pharmacol Biochem Behav. 2002 Apr;71(4):533-54.