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Adrenergički alfa-2C receptor
	; PDB prikaz baziran na 1hll.
Dostupne strukture
	1hll, 1ho9, 1hod, 1hof
Identifikatori
Simboli	ADRA2C; ADRA2L2; ADRA2RL2; ADRARL2; ALPHA2CAR
Vanjski ID	OMIM: 104250 MGI: 87936 HomoloGene: 20170 IUPHAR: α2C-adrenoceptor GeneCards: ADRA2C Gene
Ontologija gena
Molekularna funkcija	• aktivnost rodopsinu-sličnog receptora; • receptorska aktivnost; • adrenoceptorska aktivnost; • aktivnost alfa2-adrenergičkog receptora;
Celularna komponenta	• endosome; • integralno sa ćelijskom membranom; • membrana; • integralno sa membranom;
Biološki proces	• aktivacija MAPK aktivnosti; • prenos signala; • signalni put G-protein spregnutog receptora; • interćelijska signalizacija; • ponašanje;
Ortolozi

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Alfa-2C adrenergički receptor (α_2C adrenoceptor, ADRA2C) je alfa-2 adrenergički receptor. On je kodiran humanim ADRA2C genom.^[1]

Receptor

Alfa-2-adrenergički receptori su 3 visoko homologna podtipa: alfa_2A, alfa_2B, i alfa_2C. Ti receptori imaju kritičnu ulogu u regulaciji otpuštanja neurotransmitera iz simpatičkih nerva i iz adrenergičkih neurona centralnog nervnog sistema. Ispitivanja na miševima su pokazala da su oba, alfa_2A i alfa_2C, podtipa neophodna za normalnu presinaptičku kontrolu otpuštanja transmitera iz simpatičkih nerva u srcu i iz centralnih noradrenergičkih neurona. Alfa_2A podtip inhibira otpuštanje transmitera na visokim stimulacionim frekvencijama, dok alfa_2C podtip modulira neurotransmisiju na niskim nivoima nervne aktivnosti.

Gen

Ovaj gen kodira alfa2C tip receptora. On ne sadrži introne.^[1]

Ligandi

Agonisti

(R)-3-Nitrobifenilin (takođe slab antagonist α_2A i α_2B)^[2]

Antagonisti

JP-1302: selektivan u odnosu na α2A, α2B, α2D^[3]
spiroksatrin
johimbin derivati 9 i 10: >43 puta selektivniji nego za α2A, α2B i α1 tipove^[4]
N2-[4-(2,3-dihidro-benzo[1,4]dioksin-2-ilmetil)-[1,4]diazepan-1-il]-etil2-fenoksi-nikotinamid^[5]

Povezano

Adrenergički receptor

Reference

↑ ^1,0 ^1,1 „Entrez Gene: ADRA2C adrenergic, alpha-2C-, receptor”.
↑ Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, Giannella M, Paris H, Piergentili A, Quaglia W, Schaak S, Vesprini C, Pigini M (August 2007). „Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist”. Journal of Medicinal Chemistry 50 (16): 3964–8. DOI:10.1021/jm061487a. PMID 17630725.
↑ Sallinen J, Höglund I, Engström M, et al (February 2007). „Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302”. Br. J. Pharmacol. 150 (4): 391–402. DOI:10.1038/sj.bjp.0707005. PMC 2189732. PMID 17220913.
↑ Bavadekar SA, Ma G, Mustafa SM, Moore BM, Miller DD, Feller DR (November 2006). „Tethered yohimbine analogs as selective human alpha2C-adrenergic receptor ligands”. J. Pharmacol. Exp. Ther. 319 (2): 739–48. DOI:10.1124/jpet.106.105981. PMID 16873606.
↑ Patel SD, Habeski WM, Min H, et al (October 2008). „Identification and SAR around N2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist”. Bioorg. Med. Chem. Lett. 18 (20): 5689–93. DOI:10.1016/j.bmcl.2008.08.055. PMID 18799310.

Literatura

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Regan JW, Kobilka TS, Yang-Feng TL, et al. (1988). „Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype.”. Proc. Natl. Acad. Sci. U.S.A. 85 (17): 6301–5. DOI:10.1073/pnas.85.17.6301. PMC 281957. PMID 2842764.
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Chotani MA, Mitra S, Su BY, et al. (2004). „Regulation of alpha(2)-adrenoceptors in human vascular smooth muscle cells.”. Am. J. Physiol. Heart Circ. Physiol. 286 (1): H59–67. DOI:10.1152/ajpheart.00268.2003. PMID 12946937.
Small KM, Mialet-Perez J, Seman CA, et al. (2004). „Polymorphisms of cardiac presynaptic alpha2C adrenergic receptors: Diverse intragenic variability with haplotype-specific functional effects.”. Proc. Natl. Acad. Sci. U.S.A. 101 (35): 13020–5. DOI:10.1073/pnas.0405074101. PMC 516511. PMID 15319474.
Chotani MA, Mitra S, Eid AH, et al. (2005). „Distinct cAMP signaling pathways differentially regulate alpha2C-adrenoceptor expression: role in serum induction in human arteriolar smooth muscle cells.”. Am. J. Physiol. Heart Circ. Physiol. 288 (1): H69–76. DOI:10.1152/ajpheart.01223.2003. PMID 15345481.
Belfer I, Buzas B, Hipp H, et al. (2005). „Haplotype-based analysis of alpha 2A, 2B, and 2C adrenergic receptor genes captures information on common functional loci at each gene.”. J. Hum. Genet. 50 (1): 12–20. DOI:10.1007/s10038-004-0211-y. PMID 15592690.
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Vanjske veze

„α_2C-adrenoceptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-04.