Thealpha-2C adrenergic receptor (α2C adrenoceptor), also known asADRA2C, is analpha-2 adrenergic receptor, and also denotes the humangene encoding it.[5]
Alpha-2-adrenergic receptors include 3 highly homologous subtypes: alpha2A, alpha2B, and alpha2C. These receptors have a critical role in regulatingneurotransmitter release fromsympathetic nerves and from adrenergic neurons in thecentral nervous system. Studies in mice revealed that both the alpha2A and alpha2C subtypes were required for normalpresynaptic control of transmitter release from sympathetic nerves in theheart and from central noradrenergic neurons; the alpha2A subtype inhibited transmitter release at high stimulation frequencies, whereas the alpha2C subtype modulated neurotransmission at lower levels of nerve activity.[6]
^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.PMID17630725.
^Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist".Autonomic and Autacoid Pharmacology.25 (4):135–41.doi:10.1111/j.1474-8673.2005.00342.x.PMID16176444.
^Patel SD, Habeski WM, Min H, Zhang J, Roof R, Snyder B, Bora G, Campbell B, Li C, Hidayetoglu D, Johnson DS, Chaudhry A, Charlton ME, Kablaoui NM (2008). "Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist".Bioorg. Med. Chem. Lett.18 (20):5689–93.doi:10.1016/j.bmcl.2008.08.055.PMID18799310.
^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.PMID16873606.S2CID31412932.
Eason MG, Liggett SB (1993). "Human alpha 2-adrenergic receptor subtype distribution: widespread and subtype-selective expression of alpha 2C10, alpha 2C4, and alpha 2C2 mRNA in multiple tissues".Mol. Pharmacol.44 (1):70–5.PMID7688069.
Riess O, Thies U, Siedlaczck I, Potisek S, Graham R, Theilmann J, Grimm T, Epplen JT, Hayden MR (1994). "Precise mapping of the brain alpha 2-adrenergic receptor gene within chromosome 4p16".Genomics.19 (2):298–302.doi:10.1006/geno.1994.1061.PMID8188260.
Chotani MA, Mitra S, Su BY, Flavahan S, Eid AH, Clark KR, Montague CR, Paris H, Handy DE, Flavahan NA (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.PMID12946937.
Chotani MA, Mitra S, Eid AH, Han SA, Flavahan NA (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.PMID15345481.S2CID32149099.
Neumeister A, Charney DS, Belfer I, Geraci M, Holmes C, Sharabi Y, Alim T, Bonne O, Luckenbaugh DA, Manji H, Goldman D, Goldstein DS (2005). "Sympathoneural and adrenomedullary functional effects of alpha2C-adrenoreceptor gene polymorphism in healthy humans".Pharmacogenet. Genomics.15 (3):143–9.doi:10.1097/01213011-200503000-00002.PMID15861038.S2CID479475.
Park JS, Zhang SY, Jo SH, Seo JB, Li L, Park KW, Oh BH, Park YB, Kim HS (2006). "Common adrenergic receptor polymorphisms as novel risk factors for vasospastic angina".Am. Heart J.151 (4):864–9.doi:10.1016/j.ahj.2005.06.009.PMID16569551.
