Serotonin: Chimeric Protein of 5-HT2B-BRIL

PDB: http://www.rcsb.org/structure/4IB4 IUPHAR: http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=7 Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine. Drugs active at G protein-coupled receptors (GPCRs) can differentially modulate either canonical or noncanonical signaling pathways via a phenomenon known as functional selectivity or biased signaling. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system effects include neuronal sensitisation. Ergotamine is used medicinally for treatment of acute migraine attacks.