肾上腺素受体α1A

肾上腺素受体α1A
識別號
别名	ADRA1A；, ADRA1C, ADRA1L1, ALPHA1AAR, adrenoceptor alpha 1A
外部ID	OMIM：104221 MGI：104773 HomoloGene：68078 GeneCards：ADRA1A
為以下藥物的標靶
	肾上腺素、methoxamine、去甲肾上腺素、羟甲唑啉、脫羥腎上腺素、地西泮、阿夫唑嗪、bmy-7378 free base、過乳降、氯氮平、希普利敏、可迅、indoramin、ketanserin、麥角乙脲、米塞林、NAN 190、苄胺唑啉、吡貝地爾、維思通、ritanserin、roxindole、西洛多辛、spiperone、spiroxatrine、tamsulosin、定脈平、terguride、WB-4101、prazosin[1]
基因位置（人类）
染色体	染色体8（人类）[2]
终止	26,867,278 bp[2]
基因位置（小鼠）
染色体	染色体14（小鼠）[3]
终止	66,771,168 bp[3]
RNA表达模式
	; ; ; ;
	查阅更多表达数据
基因本體
分子功能	• signal transducer activity; • adrenergic receptor activity; • protein heterodimerization activity; • G-protein coupled receptor activity; • alpha1-adrenergic receptor activity; • 血浆蛋白结合;
細胞組分	• 横小管; • 核膜; • integral component of membrane; • 细胞核; • integral component of plasma membrane; • 膜; • Z disc; • 细胞膜; • 細胞質; • caveola; • dopaminergic synapse; • glutamatergic synapse; • GABA-ergic synapse; • integral component of postsynaptic membrane; • integral component of presynaptic membrane;
生物學過程	• positive regulation of cardiac muscle contraction; • negative regulation of cell proliferation; • response to hormone; • norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressure; • positive regulation of MAPK cascade; • intracellular signal transduction; • positive regulation of ERK1 and ERK2 cascade; • 訊息傳遞; • organ growth; • cell-cell signaling; • positive regulation of smooth muscle contraction; • activation of phospholipase C activity; • pilomotor reflex; • regulation of vasoconstriction; • positive regulation of heart rate; • positive regulation of synaptic transmission, GABAergic; • positive regulation of systemic arterial blood pressure; • G-protein coupled receptor signaling pathway; • 排尿; • calcium ion transport into cytosol; • positive regulation of action potential; • positive regulation of the force of heart contraction by epinephrine-norepinephrine; • 细胞凋亡; • smooth muscle contraction; • phospholipase C-activating G-protein coupled receptor signaling pathway; • adenylate cyclase-activating adrenergic receptor signaling pathway; • 老化; • regulation of cardiac muscle contraction; • positive regulation of heart rate by epinephrine-norepinephrine; • positive regulation of protein kinase C signaling; • negative regulation of Rho protein signal transduction; • regulation of muscle contraction; • response to drug; • adult heart development; • negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressure; • positive regulation of cytosolic calcium ion concentration; • positive regulation of vasoconstriction; • negative regulation of autophagy; • positive regulation of cardiac muscle hypertrophy; • positive regulation of non-membrane spanning protein tyrosine kinase activity; • cell growth involved in cardiac muscle cell development; • regulation of synaptic vesicle exocytosis; • adenylate cyclase-modulating G-protein coupled receptor signaling pathway; • neuron-glial cell signaling;
	Sources:Amigo / QuickGO
直系同源
	148
	11549
	ENSG00000120907
	ENSMUSG00000045875
	P35348
	P97718
	XM_011544412、NM_000680、NM_033302、NM_033303、NM_033304、XM_006716292、XM_006716293、XM_011544411、NM_001322502、NM_001322503、NM_001322504、NR_136343、XM_017013094、XM_017013095、XM_017013096、XR_001745476、XR_001745477
	NM_001271759、NM_001271760、NM_001271761、NM_013461、XM_006518444、XM_006518449、XM_011244923、XM_011244924、XM_011244925、XM_011244926、XM_017315800、XM_017315801、XM_017315802
	NP_000671、NP_001309431、NP_001309432、NP_001309433、NP_150645、NP_150646、NP_150647、XP_006716355、XP_006716356、XP_011542713、XP_011542714、XP_016868583、XP_016868584、XP_016868585
	NP_001258688、NP_001258689、NP_001258690、NP_038489、XP_006518507、XP_006518512、XP_011243225、XP_011243226、XP_011243227、XP_011243228、XP_017171289、XP_017171290、XP_017171291
	維基數據

肾上腺素受体α_1A（α_1A adrenoreceptor），又稱為ADRA1A[6]，是一種α1肾上腺素受体[7]。過去一度有α_1C的分類，但在研究後認為α_1C僅是α_1A的一種亞型，因此取消該命名。為了避免混淆，之後新發現的亞型便從D開始繼續命名。

受體

肾上腺素受体α₁共有3種亞型，包含α_1A、α_1B、α_1D，全都屬於Gq/11家族的G蛋白。不同亞型的致活路徑有所差異，本類受體在體內主要內源性配體為腎上腺素，主要產生战斗或逃跑反应。

基因

該蛋白的基因共有四種剪切方式，因此共有四種同型體。不同同型體可由其C端判別，但基本上功能相同[7]。

配體

致效劑

6-(5-fluoro-2-pyrimidin-5-yl-phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole: EC₅₀ = 1nM, E_max = 65%; good selectivity over α1B, α1D and α2A subtypes[8]
further partial agonistic imidazole compounds[9][10]
A-61603[11]

受體拮抗劑

Tamsulosin：用於治療良性前列腺增生症
Silodosin：用於治療良性前列腺增生症
維思通
WB-4101
Ziprasidone

在神經迴路的角色

肾上腺素受体α1A可加強對於樹樹突觸的抑制[12]。

參見

肾上腺素受体

參考文獻

.
GRCh38: Ensembl release 89: ENSG00000120907 - Ensembl, May 2017
GRCm38: Ensembl release 89: ENSMUSG00000045875 - Ensembl, May 2017
. National Center for Biotechnology Information, U.S. National Library of Medicine.
. National Center for Biotechnology Information, U.S. National Library of Medicine.
Langer SZ. . Eur. Urol. 1998,. 33 Suppl 2: 2–6. PMID 9556189. doi:10.1159/000052227.
.
Roberts LR, Fish PV, Ian Storer R, Whitlock GA. . Bioorg. Med. Chem. Lett. April 2009, 19 (11): 3113–7. PMID 19414260. doi:10.1016/j.bmcl.2009.03.166.
Whitlock GA, Brennan PE, Roberts LR, Stobie A. . Bioorg. Med. Chem. Lett. April 2009, 19 (11): 3118–21. PMID 19394220. doi:10.1016/j.bmcl.2009.03.162.
Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA. . Bioorg. Med. Chem. Lett. December 2008, 18 (24): 6437–40. PMID 18980842. doi:10.1016/j.bmcl.2008.10.066.
Knepper SM, Buckner SA, Brune ME, DeBernardis JF, Meyer MD, Hancock AA. . J. Pharmacol. Exp. Ther. 1995, 274 (1): 97–103. PMID 7616455.
Zimnik NC, Treadway T, Smith RS, Araneda RC. . J. Physiol. (Lond.). 2013, 591 (Pt 7): 1631–43. PMC 3624843. PMID 23266935. doi:10.1113/jphysiol.2012.248591.

外部連結

. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

延伸閱讀

Mátyus P, Horváth K. . Med Res Rev. 1998, 17 (6): 523–35. PMID 9359081. doi:10.1002/(SICI)1098-1128(199711)17:6<523::AID-MED2>3.0.CO;2-3.
Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT. . Hum. Mol. Genet. 1993, 1 (5): 349. PMID 1363873. doi:10.1093/hmg/1.5.349-a.
Schwinn DA, Lomasney JW, Lorenz W, 等. . J. Biol. Chem. 1990, 265 (14): 8183–9. PMID 1970822.
Hirasawa A, Shibata K, Horie K, 等. . FEBS Lett. 1995, 363 (3): 256–60. PMID 7737411. doi:10.1016/0014-5793(95)00330-C.
Diehl NL, Shreeve SM. . Eur. J. Pharmacol. 1995, 268 (3): 393–8. PMID 7805763. doi:10.1016/0922-4106(94)90064-7.
Schwinn DA, Johnston GI, Page SO, 等. . J. Pharmacol. Exp. Ther. 1995, 272 (1): 134–42. PMID 7815325.
Weinberg DH, Trivedi P, Tan CP, 等. . Biochem. Biophys. Res. Commun. 1994, 201 (3): 1296–304. PMID 8024574. doi:10.1006/bbrc.1994.1845.
Forray C, Bard JA, Wetzel JM, 等. . Mol. Pharmacol. 1994, 45 (4): 703–8. PMID 8183249.
Hirasawa A, Horie K, Tanaka T, 等. . Biochem. Biophys. Res. Commun. 1993, 195 (2): 902–9. PMID 8396931. doi:10.1006/bbrc.1993.2130.
Tseng-Crank J, Kost T, Goetz A, 等. . Br. J. Pharmacol. 1996, 115 (8): 1475–85. PMC 1908895. PMID 8564208. doi:10.1111/j.1476-5381.1995.tb16640.x.
Shibata K, Hirasawa A, Moriyama N, 等. . Br. J. Pharmacol. 1997, 118 (6): 1403–8. PMC 1909672. PMID 8832064. doi:10.1111/j.1476-5381.1996.tb15552.x.
Chang DJ, Chang TK, Yamanishi SS, 等. . FEBS Lett. 1998, 422 (2): 279–83. PMID 9490024. doi:10.1016/S0014-5793(98)00024-6.
Daniels DV, Gever JR, Jasper JR, 等. . Eur. J. Pharmacol. 1999, 370 (3): 337–43. PMID 10334511. doi:10.1016/S0014-2999(99)00154-5.
Cogé F, Guenin SP, Renouard-Try A, 等. . Biochem. J. 1999,. 343 Pt 1 (Pt 1): 231–9. PMC 1220546. PMID 10493934. doi:10.1042/0264-6021:3430231.
Rudner XL, Berkowitz DE, Booth JV, 等. . Circulation. 1999, 100 (23): 2336–43. PMID 10587338. doi:10.1161/01.cir.100.23.2336.
Ballou LM, Cross ME, Huang S, 等. . J. Biol. Chem. 2000, 275 (7): 4803–9. PMID 10671514. doi:10.1074/jbc.275.7.4803.
Keffel S, Alexandrov A, Goepel M, Michel MC. . Biochem. Biophys. Res. Commun. 2000, 272 (3): 906–11. PMID 10860850. doi:10.1006/bbrc.2000.2850.
Richman JG, Brady AE, Wang Q, 等. . J. Biol. Chem. 2001, 276 (18): 15003–8. PMID 11154706. doi:10.1074/jbc.M011679200.
Shibata K, Katsuma S, Koshimizu T, 等. . J. Biol. Chem. 2003, 278 (1): 672–8. PMID 12409310. doi:10.1074/jbc.M201375200.

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[1] .

[refGRCh38Ensembl-2] GRCh38: Ensembl release 89: ENSG00000120907 - Ensembl, May 2017

[refGRCm38Ensembl-3] GRCm38: Ensembl release 89: ENSMUSG00000045875 - Ensembl, May 2017

[4] . National Center for Biotechnology Information, U.S. National Library of Medicine.

[5] . National Center for Biotechnology Information, U.S. National Library of Medicine.

[6] Langer SZ. . Eur. Urol. 1998,. 33 Suppl 2: 2–6. PMID 9556189. doi:10.1159/000052227.

[entrez-7] .

[pmid19414260-8] Roberts LR, Fish PV, Ian Storer R, Whitlock GA. . Bioorg. Med. Chem. Lett. April 2009, 19 (11): 3113–7. PMID 19414260. doi:10.1016/j.bmcl.2009.03.166.

[pmid19394220-9] Whitlock GA, Brennan PE, Roberts LR, Stobie A. . Bioorg. Med. Chem. Lett. April 2009, 19 (11): 3118–21. PMID 19394220. doi:10.1016/j.bmcl.2009.03.162.

[pmid18980842-10] Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA. . Bioorg. Med. Chem. Lett. December 2008, 18 (24): 6437–40. PMID 18980842. doi:10.1016/j.bmcl.2008.10.066.

[pmid7616455-11] Knepper SM, Buckner SA, Brune ME, DeBernardis JF, Meyer MD, Hancock AA. . J. Pharmacol. Exp. Ther. 1995, 274 (1): 97–103. PMID 7616455.

[pmid23266935-12] Zimnik NC, Treadway T, Smith RS, Araneda RC. . J. Physiol. (Lond.). 2013, 591 (Pt 7): 1631–43. PMC 3624843. PMID 23266935. doi:10.1113/jphysiol.2012.248591.