Human HTR7

Figure. Concentration-dependent activation of HTR7 by serotonin

Reporter cells were transfected with either the expression plasmid for human 5-hydroxytryptamine receptor 7 (HTR7) or the mock plasmid and treated with various concentrations of serotonin. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 1.8 nM.

5-hydroxytryptamine receptor 7
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Psychiatry, Neurology, Musculoskeletal, Human non-orphan GPCRs

5-Hydroxytryptamine receptors

5-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]).


  1. 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.
  2. 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.
  3. 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.
  4. Ramage AG, Villalón CM. 5-hydroxytryptamine and cardiovascular regulation. Trends Pharmacol Sci 2008;29:472-81.

5-HT7 receptor

The 5-HT7 receptor is a GPCR that couples via Gs to increase cAMP production with some other transduction pathways also implicated in receptor function (e.g. ERK, Galpha12/RhoA/Cdc42). The structure displays less than 39% amino acid sequence identity to other 5-HT receptors. Several splice variants have been described.PharmacologyVarious selective 5-HT7 receptor agonists (e.g. LP-12, AS-19 [partial agonist]) and antagonists (e.g. SB 269970, SB656104-A) have been described.Clinical significanceSimilar to the 5-HT6 receptor, various non-selective psychotropic drugs also display high affinity for the 5-HT7 receptor (e.g. asenapine, clozapine, pimozide), although the consequences of this interaction are also not clear.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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