- 5-hydroxytryptamine receptor 1A
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- à la carte, Psychiatry, Neurology, Gastrointestinal, Human non-orphan GPCRs
5-Hydroxytryptamine receptors5-HT receptors are, with the exception of the ionotropic 5-HT3 class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. 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 [1,2]. Most 5-HT receptors (except 5-ht1e and 5-ht5b) play specific roles mediating functional responses in different tissues (reviewed by [3,4]).
- Bockaert J, Claeysen S, Bécamel C, et al. Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation. Cell Tissue Res 2006;326:553-72.
- Werry TD, Loiacono R, Sexton PM, et al. RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. Pharmacol Ther 2008;119:7-23.
- Villalón CM, Centurión D. Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications. Naunyn Schmiedebergs Arch Pharmacol 2007;376:45-63.
- Ramage AG, Villalón CM. 5-hydroxytryptamine and cardiovascular regulation. Trends Pharmacol Sci 2008;29:472-81.
5-HT1 receptorsThe 5-HT1 receptor family comprises five different receptors (5-HT1A, 5-HT1B, 5-HT1D, 5-ht1e, 5-HT1F), which share 40-63% amino acid sequence identity and can couple to Gi/Go to inhibit cAMP formation, although signaling via other transduction systems are known (e.g. 5-HT1A receptor activates G-protein-gated inwardly rectifying K+ channel [GIRK]). One of the 5-HT1 receptor class, the 5-ht1e receptor, is yet to achieve receptor status since a robust response mediated via the protein is yet to be reported in the literature; lower-case appellation is used to denote this. 5-HT1A and 5-HT1B receptors act as somatodendritic and terminal autoreceptors, respectively; however, these receptors are also expressed throughout the CNS.PharmacologyA number of well-defined selective agonists (e.g. 8-OH-DPAT [5-HT1A receptor], PNU 109291 [5-HT1D receptor], LY 344864 [5-HT1F receptor]) and antagonists (e.g. WAY100635 [5-HT1A receptor], SB236057 [5-HT1B receptor], SB714786 [5-HT1D receptor]), are available to selectively probe some individual members of the 5-HT1 receptors.Clinical significance5-HT1A receptors are targeted by the anxiolytic drug, buspirone, which is a partial agonist. Various ‘triptans’ (e.g. sumitriptan and zolmitriptan) are used to treat acute migraine attack, these drugs are 5-HT1B/5-HT1D receptor agonists, with some also having agonist activity at the 5-HT1F receptor.
Excerpt from IUPHAR/BPS Guide to Pharmacology
Related ReceptorsFilters Sort resultsReset Apply
Human Human Human Human Human Human Human Human Human Human Human Human Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse