5-Hydroxytryptamine Family Related Drug Discovery Products
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The brain's ability to regulate energy homeostasis is fundamentally based on the central 5-hydroxytryptamine (5-HT; serotonin) system. Nine different neuronal populations of the brain stem's raphe nuclei, which project broadly to innervate a variety of brain regions, are responsible for 5-HT production in the central nervous system (CNS). The majority of the diffuse descending projections that innervate the spinal cord, medulla, pons, and midbrain come from the caudal cell groups of the raphe. Most of the ascending projections that form a medial forebrain bundle and split out to innervate various forebrain targets originate from the rostral cell groups of the raphe.
Fig.1. 5-HT localisation and projections. (Burke & Heisler, 2015)
Creative Biolabs can offer 5-hydroxytryptamine family in vitro assays and related products with the best quality:
5-Hydroxytryptamine GPCR Assays 
GPCR Assay Kits 
GPCR Cell Lines 
GPCR Membranes 
Membrane Protein Tools
Overview of 5-Hydroxytryptamine Family
5-HT signals through seven separate kinds of 5-HT receptors (5-HTRs), which are categorized as 5-HT1R through 5-HT7R based on sequence homology and intracellular signaling pathways, when it is released at brain target locations. All 5-HTRs, with the exception of the 5-HT3R, are anticipated to have an extracellular N-terminus, seven transmembrane domains connected by three extracellular and three intracellular loops, and an intracellular C-terminus.
- 5-HT1 receptors
Similar to the rhodopsin receptor, RXFP1 and RXFP2 are family A GPCRs that specifically belong to the leucine-rich repeat-containing GPCR (LGR) subfamily. The RXFP1 and RXFP2 genes are enormous. RXFP1 and RXFP2 have 29 known splice variants, which can produce a variety of different protein products, including fragments that only have the transmembrane or extracellular region of the protein. The majority of the transmembrane-containing variants expressed at the cell surface are not ligand-binding. However, an RXFP2 variant that is only missing the exon that encodes the LDLa module can bind ligand but does not cause the production of cAMP, indicating that this variant may be a native binding protein that could modify the action of INSL3 in vivo. Therefore, by binding to and preventing relaxin from activating RXFP1, these variants might function as functional RXFP1 antagonists.
- 5-HT2 receptors
The 5-HT2 receptors saw their first thorough testing with ligands at 5-HT2A and 5-HT2C, and the involvement of 5-HT2 receptors in hallucinogenic drug action has made this a feasible method for evaluating functional selectivity in vivo. Additionally, medications that affect 5-HT2 receptors are among the most vital treatments for psychiatric conditions, some of which have serious adverse effects. Therefore, experiments focused on the 5-HT2 family account for the vast majority of data supporting functional selectivity at 5-HT receptors.
- 5-HT3 receptors
The only 5-HT receptor that is not a member of the 7TMR superfamily is 5-HT3. Electrophysiological techniques can be used to examine the properties of the 5-HT3 receptor upon binding to various ligands. Full and partial agonists caused various desensitized receptor states while targeting the same population of 5-HT3 receptors. Furthermore, it was discovered that "full and partial agonists recognize distinct conformations of unoccupied, activatable 5-HT3 receptors" during the recovery from desensitization.
- 5-HT4, 5-HT5, 5-HT6, and 5-HT7 receptors
The earliest serotonin receptors to be identified and thoroughly defined belonged to the 5-HT1 and 5-HT2 families. Thus, these receptors have provided the majority of the evidence in support of functional selectivity in the serotonergic system, in addition to having significant clinical relevance, particularly in psychiatric diseases. Such functional selectivity has yet to be fully shown for the remaining receptors. It is likely that 5-HT4, 5-HT5, 5-HT6, and 5-HT7 can also be variably recruited to cause unique physiological responses given that ligand-specific active receptor states and matching functional selectivity have been demonstrated for various receptor molecules. Therefore, these receptors are excellent candidates for further study.
Fig.2. Regulatory mechanisms of 5-HT receptors. (Stroth & Svenningsson, 2012)
References
- Burke, L.K.; Heisler, L.K. 5‐hydroxytryptamine medications for the treatment of obesity. Journal of neuroendocrinology. 2015, 27(6): 389-398.
- Stroth, N.; Svenningsson, P. Ligand‐specific differential regulation of 5‐hydroxytryptamine receptors: functional selectivity in serotonergic signaling. Wiley Interdisciplinary Reviews: Membrane Transport and Signaling. 2012, 1(4): 453-466.
