گیرنده ۵ آ سروتونین

HTR5A
معین‌کننده‌ها
نام‌های دیگر	HTR5A, 5-HT5A, 5-HT5A receptor, 5-hydroxytryptamine receptor 5A
شناسه‌های بیرونی	OMIM: 601305 MGI: 96283 HomoloGene: 22461 GeneCards: HTR5A
موقعیت ژن (موش)
کروموزوم	کروموزوم ۵ (موش)
پایان	28,060,086 bp
الگوی گسترش RNA
	More reference expression data
هستی‌شناسی ژن
عملکرد ملکولی	• G protein-coupled receptor activity; • signal transducer activity; • G protein-coupled serotonin receptor activity; • neurotransmitter receptor activity; • serotonin binding;
ترکیبات سلولی	• integral component of membrane; • پریکاریون; • پوسته یاخته; • rough endoplasmic reticulum; • دستگاه گلژی; • integral component of plasma membrane; • membrane; • دندریت; • integral component of postsynaptic specialization membrane;
فرایند زیستی	• G protein-coupled receptor signaling pathway; • G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger; • brain development; • response to estradiol; • hippocampus development; • cAMP-mediated signaling; • GO:0072468 ورارسانی پیام; • adenylate cyclase-inhibiting serotonin receptor signaling pathway; • chemical synaptic transmission;
	منابع: آمیگو / کوئیک‌گو
هم‌ساخت‌شناسی
	3361
	15563
	ENSG00000157219
	ENSMUSG00000039106
	P47898
	P30966
	NM_024012
	XM_006535631 NM_008314، XM_006535631
	NP_076917
	XP_006535694 NP_032340، XP_006535694
	مشاهده/ویرایش موش

گیرنده ۵ آ سروتونین (انگلیسی: 5-HT5A receptor) یک پروتئین است که در انسان توسط ژن «HTR5A» کًدگذاری می‌شود.

آگونیستها و آنتاگونیست‌های این گیرنده و همچنین مهارکننده‌های بازجذب سروتونین بر حسب شرایط، خاصیت تقویت‌کنندگی حافظه و/یا ضد فراموشی دارند. بخشی از عملکرد این پروتئین از طریق تنظیم تحرک کلسیم داخل‌سلولی صورت می‌پذیرد. در جوندگان این گیرندهٔ سروتونینی، دو زیرگروهِ 5-HT_5A و 5-HT_5B دارد اما در انسان با آنکه ژن کدکنندهٔ 5-HT_5B وجود دارد، اما توالی کًدگذاری‌کننده آن توسط چند کدون خاتمه گسیخته شده و این ژن را غیرفعال می‌کند. در نتیجه در انسان، تنها زیرگروه 5-HT_5A در مغز یافت می‌شود.

این گیرنده همچنین، مانند یک گیرندهٔ خودکار پیش‌سیناپسی سروتونین عمل می‌کند.

اهمیت بالینی

پیام‌رسان سروتونین در تعدادی از بیماری‌های روان‌پزشکی نقش دارد و اثرات تنگ‌کنندگی یا گشادکنندگی عروق نیز از خود نشان می‌دهد.

برخی لیگاندها

آگونیست‌ها

ال‌اس‌دی
والرنیک اسید (که از سنبل‌الطیب به‌دست می‌آید).
الانزاپین که یک آنتی‌سایکوتیک آتیپیک است.

آنتاگونیست‌ها

استلاس-۵۷۳۶
ریسپریدون (غیر انتخابی)

جستارهای وابسته

گیرنده ۴ سروتونین

منابع

↑ GRCm38: Ensembl release 89: ENSMUSG00000039106 - Ensembl, May 2017
↑ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
↑ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
↑ "Entrez Gene: HTR5A 5-hydroxytryptamine (serotonin) receptor 5A".
↑ Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M (Dec 1994). "Cloning and characterisation of the human 5-HT5A serotonin receptor". FEBS Letters. 355 (3): 242–6. doi:10.1016/0014-5793(94)01209-1. PMID 7988681. S2CID 36425845.
↑ Matthes H, Boschert U, Amlaiky N, Grailhe R, Plassat JL, Muscatelli F, Mattei MG, Hen R (Mar 1993). "Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization". Molecular Pharmacology. 43 (3): 313–9. PMID 8450829.
↑ Nelson DL (Feb 2004). "5-HT5 receptors". Current Drug Targets. CNS and Neurological Disorders. 3 (1): 53–8. doi:10.2174/1568007043482606. PMID 14965244.
↑ Thomas DR, Soffin EM, Roberts C, Kew JN, de la Flor RM, Dawson LA, Fry VA, Coggon SA, Faedo S, Hayes PD, Corbett DF, Davies CH, Hagan JJ (Sep 2006). "SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566–77. doi:10.1016/j.neuropharm.2006.04.019. PMID 16846620. S2CID 543423.
↑ The RBI Handbook of Receptor Classification and Signal Transduction, page 114 (1995)شابک ‎۰−۹۶۴۰۵۴۸−۱−۷
↑ Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (Aug 2005). "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Research. Molecular Brain Research. 138 (2): 191–7. doi:10.1016/j.molbrainres.2005.04.009. PMC 5805132. PMID 15921820.
↑ Roth BL, Driscol J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
↑ Yamazaki M, Okabe M, Yamamoto N, Yarimizu J, Harada K (2015). "Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats". J. Pharmacol. Sci. 127 (3): 362–9. doi:10.1016/j.jphs.2015.02.006. PMID 25837935.
↑ Yamazaki M, Harada K, Yamamoto N, Yarimizu J, Okabe M, Shimada T, Ni K, Matsuoka N (2014). "ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia". Eur Neuropsychopharmacol. 24 (10): 1698–708. doi:10.1016/j.euroneuro.2014.07.009. PMID 25108314.
↑ Wu J, Li Q, Bezprozvanny I (2008). "Evaluation of Dimebon in cellular model of Huntington's disease". Molecular Neurodegeneration. 3 (1): 15. doi:10.1186/1750-1326-3-15. PMC 2577671. PMID 18939977.

برای مطالعهٔ بیشتر

Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, Grewal JS, Garnovskaya MN (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction". Pharmacology & Therapeutics. 92 (2–3): 179–212. doi:10.1016/S0163-7258(01)00169-3. PMID 11916537.
Thomas DR (Sep 2006). "5-ht5A receptors as a therapeutic target". Pharmacology & Therapeutics. 111 (3): 707–14. doi:10.1016/j.pharmthera.2005.12.006. PMID 16516972.
Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M (Dec 1994). "Cloning and characterisation of the human 5-HT5A serotonin receptor". FEBS Letters. 355 (3): 242–6. doi:10.1016/0014-5793(94)01209-1. PMID 7988681. S2CID 36425845.
Schanen NC, Scherer SW, Tsui LC, Francke U (1997). "Assignment of the 5-hydroxytryptamine (serotonin) receptor 5A gene (HTR5A) to human chromosome band 7q36.1". Cytogenetics and Cell Genetics. 72 (2–3): 187–8. doi:10.1159/000134184. hdl:10722/42533. PMID 8978771.
Sanger Centre, The; Washington University Genome Sequencing Cente, The (Nov 1998). "Toward a complete human genome sequence". Genome Research. 8 (11): 1097–108. doi:10.1101/gr.8.11.1097. PMID 9847074.
Francken BJ, Josson K, Lijnen P, Jurzak M, Luyten WH, Leysen JE (May 2000). "Human 5-hydroxytryptamine(5A) receptors activate coexpressed G(i) and G(o) proteins in Spodoptera frugiperda 9 cells". Molecular Pharmacology. 57 (5): 1034–44. PMID 10779389.
Marazziti D, Ori M, Nardini M, Rossi A, Nardi I, Cassano GB (2001). "mRNA expression of serotonin receptors of type 2C and 5A in human resting lymphocytes". Neuropsychobiology. 43 (3): 123–6. doi:10.1159/000054878. PMID 11287788. S2CID 20724896.
Iwata N, Ozaki N, Inada T, Goldman D (Mar 2001). "Association of a 5-HT(5A) receptor polymorphism, Pro15Ser, to schizophrenia". Molecular Psychiatry. 6 (2): 217–9. doi:10.1038/sj.mp.4000829. PMID 11317225.
Grailhe R, Grabtree GW, Hen R (Apr 2001). "Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution". European Journal of Pharmacology. 418 (3): 157–67. doi:10.1016/S0014-2999(01)00933-5. PMID 11343685.
Noda M, Yasuda S, Okada M, Higashida H, Shimada A, Iwata N, Ozaki N, Nishikawa K, Shirasawa S, Uchida M, Aoki S, Wada K (Jan 2003). "Recombinant human serotonin 5A receptors stably expressed in C6 glioma cells couple to multiple signal transduction pathways". Journal of Neurochemistry. 84 (2): 222–32. doi:10.1046/j.1471-4159.2003.01518.x. PMID 12558985. S2CID 7364018.
Khorana N, Smith C, Herrick-Davis K, Purohit A, Teitler M, Grella B, Dukat M, Glennon RA (Aug 2003). "Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors". Journal of Medicinal Chemistry. 46 (18): 3930–7. doi:10.1021/jm030080s. PMID 12930153.
Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (Aug 2005). "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Research. Molecular Brain Research. 138 (2): 191–7. doi:10.1016/j.molbrainres.2005.04.009. PMC 5805132. PMID 15921820.

پیوند به بیرون

مکان ژنوم HTR5A انسانی و صفحهٔ جزئیات ژنی HTR5A در سامانه جستجوی بانک ژنی دانشگاه کالیفرنیا، سانتا کروز.

"5-ht_5a". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

[refGRCm38Ensembl-1] GRCm38: Ensembl release 89: ENSMUSG00000039106 - Ensembl, May 2017

[2] "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[3] "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[entrez-4] "Entrez Gene: HTR5A 5-hydroxytryptamine (serotonin) receptor 5A".

[pmid_7988681-5] Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M (Dec 1994). "Cloning and characterisation of the human 5-HT5A serotonin receptor". FEBS Letters. 355 (3): 242–6. doi:10.1016/0014-5793(94)01209-1. PMID 7988681. S2CID 36425845.

[pmid_8450829-6] Matthes H, Boschert U, Amlaiky N, Grailhe R, Plassat JL, Muscatelli F, Mattei MG, Hen R (Mar 1993). "Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization". Molecular Pharmacology. 43 (3): 313–9. PMID 8450829.

[pmid_14965244-7] Nelson DL (Feb 2004). "5-HT5 receptors". Current Drug Targets. CNS and Neurological Disorders. 3 (1): 53–8. doi:10.2174/1568007043482606. PMID 14965244.

[pmid_16846620-8] Thomas DR, Soffin EM, Roberts C, Kew JN, de la Flor RM, Dawson LA, Fry VA, Coggon SA, Faedo S, Hayes PD, Corbett DF, Davies CH, Hagan JJ (Sep 2006). "SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566–77. doi:10.1016/j.neuropharm.2006.04.019. PMID 16846620. S2CID 543423.

[9] The RBI Handbook of Receptor Classification and Signal Transduction, page 114 (1995)شابک ‎۰−۹۶۴۰۵۴۸−۱−۷

[pmid_15921820-10] Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (Aug 2005). "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Research. Molecular Brain Research. 138 (2): 191–7. doi:10.1016/j.molbrainres.2005.04.009. PMC 5805132. PMID 15921820.

[11] Roth BL, Driscol J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.

[pmid_25837935-12] Yamazaki M, Okabe M, Yamamoto N, Yarimizu J, Harada K (2015). "Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats". J. Pharmacol. Sci. 127 (3): 362–9. doi:10.1016/j.jphs.2015.02.006. PMID 25837935.

[pmid_25108314-13] Yamazaki M, Harada K, Yamamoto N, Yarimizu J, Okabe M, Shimada T, Ni K, Matsuoka N (2014). "ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia". Eur Neuropsychopharmacol. 24 (10): 1698–708. doi:10.1016/j.euroneuro.2014.07.009. PMID 25108314.

[pmid_18939977-14] Wu J, Li Q, Bezprozvanny I (2008). "Evaluation of Dimebon in cellular model of Huntington's disease". Molecular Neurodegeneration. 3 (1): 15. doi:10.1186/1750-1326-3-15. PMC 2577671. PMID 18939977.