Alpha-2C adrenergic receptor

The alpha-2C adrenergic receptor (α_2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes the human gene encoding it.^[5]

ADRA2C
Identifiers
Aliases	ADRA2C, ADRA2L2, ADRA2RL2, ADRARL2, ALPHA2CAR, adrenoceptor alpha 2C
External IDs	MGI: 87936; HomoloGene: 20170; GeneCards: ADRA2C; OMA:ADRA2C - orthologs
Gene location (Human) Chr. Chromosome 4 (human)[1] Band 4p16.3 Start 3,766,348 bp[1] End 3,768,526 bp[1]
Gene location (Mouse) Chr. Chromosome 5 (mouse)[2] Band 5 B2|5 18.09 cM Start 35,435,663 bp[2] End 35,439,107 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in decidua canal of the cervix Descending thoracic aorta ascending aorta popliteal artery tibial arteries saphenous vein vena cava right coronary artery Skeletal muscle tissue of rectus abdominis Top expressed in lumbar spinal ganglion nucleus accumbens epithelium of lens perirhinal cortex entorhinal cortex CA3 field dorsal striatum superior frontal gyrus Region I of hippocampus proper retinal pigment epithelium More reference expression data BioGPS n/a
Gene ontology Molecular function G protein-coupled receptor activity epinephrine binding protein homodimerization activity signal transducer activity adrenergic receptor activity protein binding alpha-2A adrenergic receptor binding alpha2-adrenergic receptor activity protein heterodimerization activity Cellular component cytoplasm axon terminus integral component of membrane endosome membrane plasma membrane integral component of plasma membrane axon glutamatergic synapse integral component of postsynaptic membrane integral component of postsynaptic density membrane soma Biological process G protein-coupled receptor signaling pathway activation of protein kinase B activity negative regulation of epinephrine secretion regulation of sensory perception of pain regulation of smooth muscle contraction regulation of insulin secretion female pregnancy cell-cell signaling negative regulation of norepinephrine secretion negative regulation of uterine smooth muscle contraction adenylate cyclase-activating adrenergic receptor signaling pathway regulation of vasoconstriction positive regulation of neuron differentiation positive regulation of vasoconstriction signal transduction platelet activation positive regulation of MAPK cascade adrenergic receptor signaling pathway receptor transactivation adenylate cyclase-modulating G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
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: 35.44 – 35.44 Mb PubMed search [3] [4]
Wikidata
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Receptor

Alpha-2-adrenergic receptors include 3 highly homologous subtypes: alpha_2A, alpha_2B, and alpha_2C. 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 alpha_2A and alpha_2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the alpha_2A subtype inhibited transmitter release at high stimulation frequencies, whereas the alpha_2C 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

• (R)-3-Nitrobiphenyline (also weak antagonist at α_2A and α_2B)^[7]

Antagonists

• BMY 7378 (also α_1D antagonist)^[8]
• Brexpiprazole
• JP-1302: selective over α2A, α2B, α2C^[9]
• N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide^[10]
• Pirepemat
• Quetiapine^[11]
• Risperidone
• Mirtazapine
• Spiroxatrine
• Yohimbine derivatives 9 and 10: >43 fold selectivity over α2A, α2B and α1 subtypes^[12]

See also

• Adrenergic receptor