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Adrenergički alfa-2C receptor
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
Vrsta	Čovek
Entrez	152
Ensembl	ENSG00000184160
UniProt	P18825
RefSeq (mRNA)	XM_001128592
RefSeq (protein)	XP_001128592
Lokacija (UCSC)	n/a
PubMed pretraga	[1]

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]

Vidi još

Adrenergički receptor

Reference

^ ^а ^б „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 (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. PMID 17630725. doi:10.1021/jm061487a.
^ J, Sallinen; Höglund I; Engström M (2007). „Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302”. Br. J. Pharmacol. 150 (4): 391—402. PMC 2189732 . PMID 17220913. doi:10.1038/sj.bjp.0707005.
^ Bavadekar SA, Ma G, Mustafa SM, Moore BM, Miller DD, Feller DR (2006). „Tethered yohimbine analogs as selective human alpha2C-adrenergic receptor ligands”. J. Pharmacol. Exp. Ther. 319 (2): 739—48. PMID 16873606. doi:10.1124/jpet.106.105981.
^ SD, Patel; Habeski WM; Min H (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. PMID 18799310. doi:10.1016/j.bmcl.2008.08.055.

Literatura

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