Alpha-2C adrenergic receptor

The alpha-2C adrenergic receptor2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes the human gene encoding it.[5]

ADRA2C
Identifiers
AliasesADRA2C, ADRA2L2, ADRA2RL2, ADRARL2, ALPHA2CAR, adrenoceptor alpha 2C
External IDsMGI: 87936 HomoloGene: 20170 GeneCards: ADRA2C
Orthologs
SpeciesHumanMouse
Entrez

152

11553

Ensembl

ENSG00000184160

ENSMUSG00000045318

UniProt

P18825

Q01337

RefSeq (mRNA)

NM_000683

NM_007418

RefSeq (protein)

NP_000674

NP_031444

Location (UCSC)Chr 4: 3.77 – 3.77 MbChr 5: 35.44 – 35.44 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Receptor

Alpha-2-adrenergic receptors include 3 highly homologous subtypes: alpha2A, alpha2B, and alpha2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mice revealed that both the alpha2A and alpha2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart 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]

Gene

This gene encodes the alpha2C subtype, which contains no introns in either its coding or untranslated sequences.[5]

Ligands

Agonists

Antagonists

See also

References

  1. GRCh38: Ensembl release 89: ENSG00000184160 - Ensembl, May 2017
  2. GRCm38: Ensembl release 89: ENSMUSG00000045318 - Ensembl, May 2017
  3. "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. "Entrez Gene: ADRA2C adrenergic, alpha-2C-, receptor".
  6. "ADRA2C adrenoceptor alpha 2C [Homo sapiens (human)] - Gene - NCBI". www.ncbi.nlm.nih.gov. Retrieved 2018-09-11.
  7. 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.
  8. 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. PMID 16176444.
  9. Sallinen J, Höglund I, Engström M, Lehtimäki J, Virtanen R, Sirviö J, Wurster S, Savola JM, Haapalinna A (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.
  10. 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. PMID 18799310.
  11. Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL (September 2008). "N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity". Neuropsychopharmacology. 33 (10): 2303–12. doi:10.1038/sj.npp.1301646. PMID 18059438.
  12. 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. S2CID 31412932.

Further reading

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