Insights into the structure and function of 5-HT(2) family serotonin receptors reveal novel strategies for therapeutic target development
by
Roth BL, Shapiro DA.
Departments of Biochemistry, Neurosciences and Psychiatry,
Case Western Reserve University Medical School,
10900 Euclid Avenue, Cleveland, Ohio, 44106-4935, USA.
roth@biocserver.cwru.edu
Expert Opin Ther Targets 2001 Dec;5(6):685-695


ABSTRACT

5-HT(2) family serotonin receptors, principal sites of action of serotonin in the brain, represent major molecular targets for drugs used in treating a variety of diseases including schizophrenia, depression, anxiety, eating disorders, obsessive-compulsive disorder, chronic pain conditions and obesity. The 5-HT(2) family of receptors has three members: 5-HT(2A), 5-HT(2B) and 5-HT(2C). Therefore, it is likely that subtype-selective compounds will be needed to avoid serious side effects and to enhance therapeutic indices. Unfortunately, recent insights into the structure and function of 5-HT(2A) receptors have revealed that structurally-diverse agonists and antagonists have distinct modes of interacting with 5-HT(2A) receptors, complicating efforts at structure-based drug-design. These distinct binding modes would not have been predicted based on conventional structure-activity relationships or static docking models. Fortunately, these complicated binding modes can be predicted and simulated using molecular dynamics, allowing for the possibility of structure-based drug design. Thus, provided appropriately sophisticated drug design strategies are employed, it is likely that uniquely valuable medications will result which could have great potential for treating a variety of mental and physical illnesses.
SSRIs
5-HT2
5-HT3
5-HT1a
5-HT1b
5-HT1d
5-HT2a
5-HT2c
Mianserin
Flibanserin
Mirtazapine
Desipramine
MDMA/5-HT2
5-HT2c/5-HT2b
Serotonergic drugs
5-HT2a antagonists
Serotonin 5-HT2c receptors
Depression, SSRIs and the serotonin 5-HT2 receptors


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