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2 Citations
Facts about 5-hydroxytryptamine receptor 1B.
Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling through G proteins and mediate activation of alternative signaling pathways.
Human | |
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Gene Name: | HTR1B |
Uniprot: | P28222 |
Entrez: | 3351 |
Belongs to: |
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G-protein coupled receptor 1 family |
5HT1B; 5-HT1B; 5-HT1B5-HT-1B; 5HT1DB; 5-HT1DB; 5-hydroxytryptamine (serotonin) receptor 1B; HTR1B; HTR1D2; HTR1D2,5-hydroxytryptamine receptor 1B; HTR1DB; S12; S125-HT-1D-beta; Serotonin 1D beta receptor; Serotonin receptor 1B
Mass (kDA):
43.568 kDA
Human | |
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Location: | 6q14.1 |
Sequence: | 6; NC_000006.12 (77460924..77463491, complement) |
Detected in cerebral artery smooth muscle cells (at protein level). Detected in brain cortex, striatum, amygdala, medulla, hippocampus, caudate nucleus and putamen.
Cell membrane; Multi-pass membrane protein.
If you've ever wondered about the various uses of the HTR1B marker, you're not alone. Several scientists worldwide have benefited from this product. These scientists use HTR1B to discover how species or applications react to various compounds. They can also submit results from special samples for product credits. The best part is that these credits are valid for all scientists in the world.
As a class I ligand for the 5-HTR1B G-protein coupled receptor, ergot alkaloid derivatives have a diverse range of biological functions. In animals, they act as receptors for serotonin and various anxiolytic drugs. These agents also modulate the activity of downstream effectors, including the adenylate cyclase enzyme.
The ergot alkaloid derivatives, such as methyllergonovine, are derived from ergot. They act as alpha-adrenergic antagonists and are widely used for treating migraine headaches, the symptoms of cerebrovascular abnormalities, and cognitive decline in older adults. In addition, they are also used to treat hemorrhage in patients with uterine atony and postpartum hemorrhage.
The primary toxicological effect of ergot alkaloid is vasoconstriction and hypoprolactinaemia. Intoxication of equines can cause poor weight gain, reduced fertility, hyperthermia, convulsions, and death. Therefore, the regulatory framework for seed certification should include ergot alkaloid testing. For equine purposes, ergot alkaloid from pasture grass can adversely affect animal health and performance.
The ergot alkaloid is a secondary metabolite produced by certain fungi. It has been isolated from four species of the Clavicipitaceae family, including C. purpurea, which lives mostly on cereals. Other species such as Neotyphodium infect forages and tall fescue. The ergot alkaloids are substituted on the C-8 atom of the pyrophosphate moiety.
We tested whether HTR1B is a receptor for the lysergic acid diethynamide. We used membrane preparations from HEK293 T cells transiently expressing HTR2A and ligands to target these proteins. Binding was performed in 96-well plates containing standard binding buffer (50 mM Tris, 0.1 mM EDTA, 10 mM MgCl2), 1% BSA, and 0.01% ascorbic acid.
Different combinations of Htrs are expressed in different areas of the brain. Htr1a is expressed in dentate gyrus granule cells while Htr1b is expressed in layer II pyramidal cells. Htr7 and Htr2a are expressed in GADth interneurons, and Htr2a is present in the mossy cells of the hilus.
The 5-HT receptor is a G-protein-coupled protein (GPCR). It binds to lysergic acid diethylic acid (DOI) and various drugs. The 5-HT receptor family also includes the 5-HT1B receptor. The activity of the 5-HT receptor is mediated through G proteins and adenylate cyclase.
The expression patterns of several Htrs have been studied in mouse hippocampus. Several studies have suggested that Htr1a and Htr2a are expressed differently in ventral hippocampus and contribute to different aspects of learning and memory. The enrichment of Htr1a and Htr2a in the ventral hippocampus suggests that these receptors may play a role in mood and anxiety-related behaviour. Further, Htr1a and Htr2a may be involved in antidepressant properties of SSRIs.
The antiserum for human HTR1B was purified by peptide affinity chromatography. Using a SulfoLinkTM Coupling Resin, the antiserum was identified as a synthetic peptide derived from human 5HT1B Receptor corresponding to its internal amino acids. In addition, it contained sodium azide for anti-microbial activity.
The activity of HTR1B is related to the release of catecholamine from adrenal medulla and control of the brain's temperature. Moreover, it affects the sensitivity of nerve cells to anxiogenic stimuli, such as stress. This receptor also has a role in glucose homeostasis and insulin sensitivity. This makes it a prime candidate for treating anxiotropic disorders.
PMID: 1315531 by Hamblin M.W., et al. Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5- HT1D-like pharmacological specificity.
PMID: 1610347 by Mochizuki D., et al. Cloning and expression of the human 5-HT1B-type receptor gene.
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