More information on this family may be found on the IUPHAR-DB family and introduction pages.
5-HT receptors [nomenclature as agreed by NC-IUPHAR Subcommittee on 5-HT receptors [46] and subsequently revised [41]] are, with the exception of the ionotropic 5-HT3 class, GPCR receptors where the endogenous agonist is 5-HT. The diversity of metabotropic 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT2A (non-functional), 5-HT2C (non-functional), 5-HT4, 5-HT6 (non-functional) and 5-HT7 receptors. Unique amongst the GPCRs, RNA editing produces 5-HT2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to Gq/11 and also pharmacology [11,109]. Most 5-HT receptors (except 5-ht 1e and 5-ht 5a/5b) play specific roles mediating functional responses in different tissues (reviewed by [89,104].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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Tabulated pKi and KD values refer to binding to human 5-HT receptors unless indicated otherwise. Unreferenced values are extracted from the NC-IUPHAR database (www.iuphar-db.org). The nomenclature of 5-HT1B/5-HT1D receptors has been revised [41]. Only the non-rodent form of the receptor was previously called 5-HT1D;: the human 5-HT1B receptor (tabulated) displays a different pharmacology to the rodent forms of the receptor due to Thr335 of the human sequence being replaced by Asn in rodent receptors. NAS181 is a selective antagonist of the rodent 5-HT1B receptor. fananserin and ketanserin bind with high affinity to dopamine D4 and histamine H1 receptors respectively, and ketanserin is a potent α1 adrenoceptor antagonist, in addition to blocking 5-HT2A receptors. The human 5-ht5A receptor has been claimed to couple to several signal transduction pathways when stably expressed in C6 glioma cells [83]. The human orthologue of the mouse 5-ht5b receptor is non-functional due to interruption of the gene by stop codons. The 5-ht1e receptor appears not to have been cloned from mouse, or rat, impeding definition of its function. In addition to the receptors listed in the table, an 'orphan' receptor, unofficially termed 5-HT1P, has been described [35].