Serotonin: Chimeric Protein of 5-HT2B-BRIL

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PDB: http://www.rcsb.org/structure/4IB4 IUPHAR: http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=7 The crystal structure reveals a chimeric protein composed of 5-HT2B-BRIL in complex with ergotamine. Drugs that target G protein-coupled receptors can selectively activate either conventional or unconventional signaling pathways by exploiting the concept of functional selectivity or biased signaling. The 5-HT2 family of receptors, which includes the 5-HT2B subtype, plays a key role in regulating various physiological functions of serotonin both centrally and peripherally. These effects on the cardiovascular system include blood vessel constriction and platelet shape changes; central nervous system effects involve heightened neuronal sensitivity. Ergotamine is medically employed to treat acute migraine episodes.