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、甲氧明、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、過乳降、氯氮平、希普利敏、可迅、indoramin、酮色林、麥角乙脲、米塞林、NAN 190、苄胺唑啉、吡貝地爾、利培酮、ritanserin、roxindole、赛洛多辛、spiperone、spiroxatrine、坦索羅辛、定脈平、特麦角脲、WB-4101、哌唯嗪、異蘇氨酸、肾上腺素、去甲肾上腺素、麻黃鹼、methoxamine hydrochloride、dabuzalgron、dipivefrin hydrochloride、多沙唑嗪甲磺酸盐、oxymetazoline hydrochloride、phenoxybenzamine hydrochloride、phenylephrine hydrochloride、prazosin hydrochloride、tamsulosin hydrochloride、midodrine hydrochloride、alfuzosin hydrochloride[1]
基因位置（人类）
染色体	8號染色體[2]
终止	26,867,278 bp[2]
基因位置（小鼠）
染色体	小鼠14号染色体[3]
终止	67,008,617 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 population 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; • 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
NM_000680; NM_033302; NM_033303; NM_033304; NM_001322502;
	NM_001322503; NM_001322504
	NM_001271759; NM_001271760; NM_001271761; NM_013461
NP_000671; NP_001309431; NP_001309432; NP_001309433; NP_150645;
	NP_150646; NP_150647
	NP_001258688; NP_001258689; NP_001258690; NP_038489
	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

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.
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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. （原始内容存档于2020-11-22）.

延伸閱讀

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[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.