Alpha-2C adrenergic receptor

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Adrenoceptor alpha 2C
Protein ADRA2C PDB 1hll.png
PDB rendering based on 1hll.
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols ADRA2C ; ADRA2L2; ADRA2RL2; ADRARL2; ALPHA2CAR
External IDs OMIM104250 MGI87936 HomoloGene20170 IUPHAR: α2C-adrenoceptor ChEMBL: 1916 GeneCards: ADRA2C Gene
Orthologs
Species Human Mouse
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 Mb
Chr 5:
35.28 – 35.28 Mb
PubMed search [1] [2]

The alpha-2C adrenergic receptor2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes the human gene encoding it.[1]

Receptor[edit]

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.

Gene[edit]

This gene encodes the alpha2C subtype, which contains no introns in either its coding or untranslated sequences.[1]

Ligands[edit]

Antagonists

BMY 7378 (also α1D antagonist)[2]

Ligands[edit]

Agonists[edit]

Antagonists[edit]

  • JP-1302: selective over α2A, α2B, α2C[4]
  • spiroxatrine
  • yohimbine derivatives 9 and 10: >43 fold selectivity over α2A, α2B and α1 subtypes[5]
  • N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide[6]

See also[edit]

References[edit]

  1. ^ a b "Entrez Gene: ADRA2C adrenergic, alpha-2C-, receptor". 
  2. ^ Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist". Auton Autacoid Pharmacol 25 (4): 135–41. doi:10.1111/j.1474-8673.2005.00342.x. PMID 16176444. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ Patel SD, Habeski WM, Min H, et al (October 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. 

Further reading[edit]