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The Multiplicity of Serotonin Receptors: Uselessly Diverse Molecules or an Embarrassment of Riches?

Department of Psychiatry, Department of Biochemistry, Department of Neuroscience, Case Western Reserve University Medical School, Cleveland, Ohio, roth{at}biocserver.cwru.edu

Estelle Lopez

Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, Ohio

Shamil Patel

Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, Ohio

Wesley K. Kroeze

Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, Ohio

A large number of 5-HT receptors (>15) have been identified by molecular cloning technology over the past 10 years. This review briefly summarizes available information regarding the functional and therapeutic implications of serotonin receptor diversity for neurology and psychiatry. 5-HT receptors are divided into seven main families: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, and 5-HT7. Several families (e.g., 5-HT1 family) have many members (e.g., 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT1F), each of which is encoded by a distinct gene product. In addition to the genomic diversity of 5-HT receptors, splice variants and editing isoforms exist for many of the 5-HT receptors, making the family even more diverse. Evidence that is summarized in this review suggests that 5-HT receptors represent novel therapeutic targets for a number of neurologic and psychiatric diseases including migraine headaches, chronic pain conditions, schizophrenia, anxiety, depression, eating disorders, obsessive compulsive disorder, pervasive developmental disorders, and obesity-related conditions (Type II diabetes, hypertension, obesity syndromes). It is possible that sub-type-selective serotonergic agents may revolutionize the treatment for a number of medical, psychiatric, and neurological disorders.

Key Words: Serotonin receptors • Antidepressant • Antipsychotic • Clozapine • Fluoxetine

The Neuroscientist, Vol. 6, No. 4, 252-262 (2000)
DOI: 10.1177/107385840000600408


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