Human Serotonin 5-HT G Protein-Coupled Receptor Homology Model from the Adrenoceptor Structure: Ligand Docking and Mutagenesis Studies.

Activation of the serotonin (5-hydroxytryptamine, 5-HT) 5HT G protein-coupled receptor (GPCR) is proposed as novel pharmacotherapy for obesity and neuropsychiatric disorders. In contrast, activation of the 5-HT and 5-HT GPCRs is associated with untoward hallucinogenic and cardiopulmonary effects, respectively. There is no crystal structure available to guide design of 5-HT receptor-specific ligands.