5-HT1B receptor

• 5-HT1B受容体、5-HT1Bレセプター、セロトニン1B受容体、セロトニン1Bレセプター

関

serotonin receptor

WordNet

1. a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

1. =sense organ / 受信装置

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/25 05:53:03」(JST)

wiki en

[Wiki en表示]

5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled
Available structures PDB Ortholog search: PDBe, RCSB List of PDB id codes 4IAQ, 4IAR
Identifiers
Symbols	HTR1B; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12
External IDs	OMIM: 182131 MGI: 96274 HomoloGene: 669 IUPHAR: 5-HT1B ChEMBL: 1898 GeneCards: HTR1B Gene
Gene Ontology Molecular function • serotonin receptor activity • drug binding • serotonin binding Cellular component • cytoplasm • plasma membrane • integral to plasma membrane Biological process • G-protein coupled receptor internalization • G-protein coupled receptor signaling pathway • G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger • protein kinase C-activating G-protein coupled receptor signaling pathway • synaptic transmission • regulation of dopamine secretion • negative regulation of cAMP biosynthetic process • negative regulation of synaptic transmission, GABAergic • response to cocaine • vasoconstriction • response to drug • drinking behavior • response to ethanol • bone remodeling • regulation of behavior • response to mineralocorticoid stimulus • negative regulation of synaptic transmission, glutamatergic • cellular response to temperature stimulus Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	3351	15551
Ensembl	ENSG00000135312	ENSMUSG00000049511
UniProt	P28222	P28334
RefSeq (mRNA)	NM_000863	NM_010482
RefSeq (protein)	NP_000854	NP_034612
Location (UCSC)	Chr 6: 78.17 – 78.17 Mb	Chr 9: 81.63 – 81.63 Mb
PubMed search	[1]	[2]

5-hydroxytryptamine receptor 1B also known as the 5-HT_1B receptor is a protein that in humans is encoded by the HTR1B gene. The 5-HT_1B receptor is a 5-HT receptor subtype.

Tissue distribution and function

5-HT_1B receptors are widely distributed throughout the CNS with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the 5-HT_1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inhibiting the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency, respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT_1B heteroreceptors produces a facilitation in excitatory synaptic transmission which is altered in depression.

Outside the brain, 5-HT_1B receptor activation also has vascular effects, such as pulmonary vasoconstriction. Furthermore, blocking 5-HT_1B receptor signaling decreases the number of osteoblasts, bone mass, and the bone formation rate.

Knockout mice lacking the 5-HT_1B gene have shown an increase in aggression and a higher preference for alcohol. Under basal conditions, knockout mice present with a "normal" phenotype and a exhibit a sucrose preference (a measure of anhedonia). However, after undergoing chronic unpredictable stress treatment to induce a "depression-like" phenotype these animals do not benefit from administration of selective serotonin reuptake inhibitor (SSRIs).

Ligands

Agonists

• ergotamine (vasoconstrictor in migraine)
• sumatriptan (vasoconstrictor in migraine)
• zolmitriptan
• 5-Carboxamidotryptamine
• CGS-12066A
• CP-93,129 (peripherally acting)
• CP-94,253
• CP-135,807 (mixed 5-HT_1B/1D agonist)
• RU-24969 (mixed 5-HT_1A/1B agonist)

Partial agonists

• Vortioxetine (antidepressant)

Antagonists and inverse agonists

• methiothepin (antipsychotic)
• yohimbine (aphrodisiac)
• metergoline
• isamoltane
• AR-A000002
• SB-216,641
• SB-224,289 (inverse agonist)
• SB-236,057 (inverse agonist)

Genetics

In humans the protein is coded by the gene HTR1B.

A genetic variant in the promotor region, A-161T, has been examined with respect to personality traits and showed no major effect.

See also

• 5-HT₁ receptor
• 5-HT receptor

References

External links

• "5-HT_1B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

• Olivier B, van Oorschot R (2006). "5-HT1B receptors and aggression: a review.". Eur. J. Pharmacol. 526 (1–3): 207–17. doi:10.1016/j.ejphar.2005.09.066. PMID 16310769. 
• Hamblin MW, Metcalf MA, McGuffin RW, Karpells S (1992). "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". Biochem. Biophys. Res. Commun. 184 (2): 752–9. doi:10.1016/0006-291X(92)90654-4. PMID 1315531. 
• Veldman SA, Bienkowski MJ (1992). "Cloning and pharmacological characterization of a novel human 5-hydroxytryptamine1D receptor subtype". Mol. Pharmacol. 42 (3): 439–44. PMID 1328844. 
• Demchyshyn L, Sunahara RK, Miller K, et al. (1992). "A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6". Proc. Natl. Acad. Sci. U.S.A. 89 (12): 5522–6. doi:10.1073/pnas.89.12.5522. PMC 49324. PMID 1351684. 
• Levy FO, Gudermann T, Perez-Reyes E, et al. (1992). "Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype". J. Biol. Chem. 267 (11): 7553–62. PMID 1559993. 
• Weinshank RL, Zgombick JM, Macchi MJ, et al. (1992). "Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta". Proc. Natl. Acad. Sci. U.S.A. 89 (8): 3630–4. doi:10.1073/pnas.89.8.3630. PMC 48922. PMID 1565658. 
• Mochizuki D, Yuyama Y, Tsujita R, et al. (1992). "Cloning and expression of the human 5-HT1B-type receptor gene". Biochem. Biophys. Res. Commun. 185 (2): 517–23. doi:10.1016/0006-291X(92)91655-A. PMID 1610347. 
• Nöthen MM, Erdmann J, Shimron-Abarbanell D, Propping P (1995). "Identification of genetic variation in the human serotonin 1D beta receptor gene". Biochem. Biophys. Res. Commun. 205 (2): 1194–200. doi:10.1006/bbrc.1994.2792. PMID 7802650. 
• Ng GY, George SR, Zastawny RL, et al. (1993). "Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition". Biochemistry 32 (43): 11727–33. doi:10.1021/bi00094a032. PMID 8218242. 
• Bouchelet I, Cohen Z, Case B, et al. (1996). "Differential expression of sumatriptan-sensitive 5-hydroxytryptamine receptors in human trigeminal ganglia and cerebral blood vessels". Mol. Pharmacol. 50 (2): 219–23. PMID 8700126. 
• Varnäs K, Hall H, Bonaventure P, Sedvall G (2001). "Autoradiographic mapping of 5-HT(1B) and 5-HT(1D) receptors in the post mortem human brain using [(3)H]GR 125743". Brain Res. 915 (1): 47–57. doi:10.1016/S0006-8993(01)02823-2. PMID 11578619. 
• Salim K, Fenton T, Bacha J, et al. (2002). "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation". J. Biol. Chem. 277 (18): 15482–5. doi:10.1074/jbc.M201539200. PMID 11854302. 
• Hasegawa Y, Higuchi S, Matsushita S, Miyaoka H (2002). "Association of a polymorphism of the serotonin 1B receptor gene and alcohol dependence with inactive aldehyde dehydrogenase-2". Journal of neural transmission (Vienna, Austria : 1996) 109 (4): 513–21. doi:10.1007/s007020200042. PMID 11956970. 
• Hawi Z, Dring M, Kirley A, et al. (2003). "Serotonergic system and attention deficit hyperactivity disorder (ADHD): a potential susceptibility locus at the 5-HT(1B) receptor gene in 273 nuclear families from a multi-centre sample". Mol. Psychiatry 7 (7): 718–25. doi:10.1038/sj.mp.4001048. PMID 12192616. 
• Mammalian Gene Collection Program Team; Strausberg, R. L.; Feingold, E. A.; Grouse, L. H. et al. (2002). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proceedings of the National Academy of Sciences 99 (26): 16899–16903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932. 
• Huang YY, Oquendo MA, Friedman JM, et al. (2003). "Substance abuse disorder and major depression are associated with the human 5-HT1B receptor gene (HTR1B) G861C polymorphism". Neuropsychopharmacology 28 (1): 163–9. doi:10.1038/sj.npp.1300000. PMID 12496953. 
• Quist JF, Barr CL, Schachar R, et al. (2003). "The serotonin 5-HT1B receptor gene and attention deficit hyperactivity disorder". Mol. Psychiatry 8 (1): 98–102. doi:10.1038/sj.mp.4001244. PMID 12556913. 
• Sinha R, Cloninger CR, Parsian A (2003). "Linkage disequilibrium and haplotype analysis between serotonin receptor 1B gene variations and subtypes of alcoholism". Am. J. Med. Genet. B Neuropsychiatr. Genet. 121 (1): 83–8. doi:10.1002/ajmg.b.20064. PMID 12898580. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 小児や青年の注意欠陥多動性障害：疫学および病因 attention deficit hyperactivity disorder in children and adolescents epidemiology and pathogenesis
• 2. 冠動脈内皮細胞機能不全：基本概念 coronary artery endothelial dysfunction basic concepts
• 3. セロトニンモジュレータ：薬理学、投与、および副作用 serotonin modulators pharmacology administration and side effects
• 4. 小児における片頭痛の病態生理、臨床的特徴、および診断 pathophysiology clinical features and diagnosis of migraine in children
• 5. 成人における片頭痛の病態生理、臨床症状、および診断 pathophysiology clinical manifestations and diagnosis of migraine in adults

English Journal

• Effect of chronic treatment with angiotensin type 1 receptor antagonists on striatal dopamine levels in normal rats and in a rat model of Parkinson's disease treated with l-DOPA.

• Dominguez-Meijide A, Villar-Cheda B, Garrido-Gil P, Sierrra-Paredes G, Guerra MJ, Labandeira-Garcia JL.SourceLaboratory of Neuroanatomy and Experimental Neurology, Department of Morphological Sciences, Faculty of Medicine, University of Santiago de Compostela, Santiago de Compostela, Spain; Networking Research Center on Neurodegenerative Diseases (CIBERNED), Spain.
• Neuropharmacology.Neuropharmacology.2014 Jan;76 Pt A:156-68. doi: 10.1016/j.neuropharm.2013.07.016. Epub 2013 Aug 20.
• Beneficial effects of angiotensin type-1 receptor (AT1) inhibition have been observed in a number of brain processes mediated by oxidative stress and neuroinflammation, including Parkinson's disease. However, important counterregulatory interactions between dopamine and angiotensin systems have rece
• PMID 23973568

• Peripheral and spinal 5-HT receptors participate in the pronociceptive and antinociceptive effects of fluoxetine in rats.

• Cervantes-Durán C, Rocha-González HI, Granados-Soto V.SourceDepartamento de Farmacobiología, Centro de Investigación y de Estudios Avanzados (Cinvestav), Sede Sur, México, D.F., Mexico.
• Neuroscience.Neuroscience.2013 Nov 12;252:396-409. doi: 10.1016/j.neuroscience.2013.08.022. Epub 2013 Aug 27.
• The role of 5-HT receptors in fluoxetine-induced nociception and antinociception in rats was assessed. Formalin produced a typical pattern of flinching and licking/lifting behaviors. Local peripheral ipsilateral, but not contralateral, pre-treatment with fluoxetine (0.3-3nmol/paw) increased in a dos
• PMID 23994595

• Altered somatosensory barrel cortex refinement in the developing brain of Mecp2-null mice.

• Moroto M, Nishimura A, Morimoto M, Isoda K, Morita T, Yoshida M, Morioka S, Tozawa T, Hasegawa T, Chiyonobu T, Yoshimoto K, Hosoi H.SourceDepartment of Pediatrics, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 465 Kajii-cho, Kawaramachi-Hirokoji, Kamigyo-ku, Kyoto 602-8566, Japan. Electronic address: moroto@koto.kpu-m.ac.jp.
• Brain research.Brain Res.2013 Nov 6;1537:319-26. doi: 10.1016/j.brainres.2013.09.017. Epub 2013 Sep 21.
• Rett syndrome (RTT) is a neurodevelopmental disorder caused by mutations in the methyl-CpG binding protein 2 (MeCP2) gene. In previous studies, monoaminergic dysfunctions have been detected in patients with RTT and in a murine model of RTT, the Mecp2-null mouse. Therefore, the pathogenesis of RTT is
• PMID 24060648

Japanese Journal

• Pathology and Neurotoxicity in Dogs after Repeat Dose Exposure to a Serotonin 5-HT1B Inhibitor

• CHANG Jane C.F.,CIACCIO Paul,SCHROEDER Patricia,WRIGHT Lindsay,WESTWOOD Russell,BERG Anna-Lena
• Journal of Toxicologic Pathology, 2013
• … AZD3783, a cationic amphiphilic drug and a potent inhibitor of the 5-hydroxytryptamine (5-HT1B) receptor, was explored as a potential treatment for depression. …
• NAID 130003382471

• Sarpogrelate Dilates Cerebral Arteries in the Absence of Exogenous Serotonin

• KAWAMURA Maiko,ISHIGURO Masanori,NAGAMINE Takashi,HOUKIN Kiyohiro
• Neurologia medico-chirurgica 53(5), 291-298, 2013
• … Vasoconstriction of arteries induced by serotonin (5-hydroxytryptamine: 5-HT) is mediated by 5-HT2A and 5-HT1B receptors localized on smooth muscle. … The present study investigated the impact of sarpogrelate, a 5-HT2A receptor antagonist, on cerebral artery diameter in the presence and absence of exogenous 5-HT. …
• NAID 130003364247

• Pathophysiologic Basis of Anorexia: Focus on the Interaction between Ghrelin Dynamics and the Serotonergic System

• Takeda Hiroshi,Nakagawa Koji,Okubo Naoto,Nishimura Mie,Muto Shuichi,Ohnishi Shunsuke,Sakamoto Naoya,Hosono Hidetaka,Asaka Masahiro
• Biological and Pharmaceutical Bulletin 36(9), 1401-1405, 2013
• … Cisplatin-induced anorexia is attributable to a decrease in peripheral and central ghrelin secretion caused by the stimulation of serotonin (5-hydroxytryptamine; … 5-HT)2B and 5-HT2C receptors via 5-HT secretion. …
• NAID 130003361528

Related Links

• 5-HT1B receptor - wikidoc

5-HT1B receptor Jump to: navigation, search The correct title of this article is 5-HT 1B receptor. It appears incorrectly here because of technical restrictions. 5-hydroxytryptamine (serotonin) receptor 1B Identifiers Symbol(s) HTR1B ...

• The 5-HT1B receptor - MDMA / Ecstasy : Utopian Pharmacology

The 5-HT1B receptor: behavioral implications by Clark MS, Neumaier JF. Department of Psychiatry and Behavioral Sciences, Harborview Medical Center, University of Washington, Seattle, USA. Psychopharmacol Bull 2001 Autumn ...

Related Pictures

---

★リンクテーブル★

リンク元	「serotonin receptor」「5-HT1B受容体」「5-HT1Bレセプター」「セロトニン1B受容体」「セロトニン1Bレセプター」
関連記事	「HT」

「serotonin receptor」

　　[★]

• セロトニン受容体、セロトニンレセプター

関

5-HT receptor、5-HT1A receptor、5-HT1A serotonin receptor、5-HT1B receptor、5-HT2A receptor、5-HT2C receptor、5-HT3 receptor

「5-HT1B受容体」

　　[★]

英

5-HT1B receptor

関

5-HT1Bレセプター、セロトニン1Bレセプター、セロトニン1B受容体

「5-HT1Bレセプター」

　　[★]

英

5-HT1B receptor

関

5-HT1B受容体、セロトニン1Bレセプター、セロトニン1B受容体

「セロトニン1B受容体」

　　[★]

英

5-HT1B receptor

関

5-HT1B受容体、5-HT1Bレセプター、セロトニン1Bレセプター

「セロトニン1Bレセプター」

　　[★]

英

5-HT1B receptor

関

5-HT1B受容体、5-HT1Bレセプター、セロトニン1B受容体

「HT」

　　[★]

• 高血圧症 高血圧 hypertension
• 心移植 heart transplantation