Alpha-2C adrenergic receptor
Also known as: ADRA2C, ADRA2L2, ADRA2RL2
Function
Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate the G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression. Control a variety of physiological processes, such as regulation of blood pressure, lipolysis and insulin release. ADRA2A and ADRA2C mediates the presynaptic feedback inhibition of neurotransmitter release from noradrenergic nerve terminals in sympathetic and central nervous systems. ADRA2A inhibits transmitter release at high stimulation frequencies, whereas ADRA2C modulates neurotransmission at lower levels of nerve activity (By similarity). The rank order of potency for physiological agonists of ADRA2C is epinephrine > norepinephrine > dopamine.
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- ADR_fam, ADRA2C_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
- Functional cluster
- Nucleic Acid Metabolism & Repair Enzymes
Experimental structures · PDB · 1
- 6KUW X-ray 2.80A
A predicted model is available from AlphaFold.
Gene Ontology · 22
- GO:0005737 cytoplasm
- GO:0005768 endosome
- GO:0005886 plasma membrane
- GO:0031694 alpha-2A adrenergic receptor binding
- GO:0004938 alpha2-adrenergic receptor activity
- GO:0051379 epinephrine binding
- GO:0046982 protein heterodimerization activity
- GO:0042803 protein homodimerization activity
- GO:0071881 adenylate cyclase-inhibiting adrenergic receptor signaling pathway
- GO:0071875 adrenergic receptor signaling pathway
- GO:0007267 cell-cell signaling
- GO:0007173 epidermal growth factor receptor signaling pathway
- GO:0007186 G protein-coupled receptor signaling pathway
- GO:0032811 negative regulation of epinephrine secretion
- GO:0046676 negative regulation of insulin secretion
- GO:0010700 negative regulation of norepinephrine secretion
- GO:0030168 platelet activation
- GO:0043410 positive regulation of MAPK cascade
- GO:0045666 positive regulation of neuron differentiation
- GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- GO:0006940 regulation of smooth muscle contraction
- GO:0019229 regulation of vasoconstriction
Drugs targeting this protein · 40
- IDAZOXAN antagonist
- LABETALOL HYDROCHLORIDE antagonist
- TIZANIDINE HYDROCHLORIDE agonist
- APRACLONIDINE HYDROCHLORIDE agonist
- BRIMONIDINE TARTRATE agonist
- TETRAHYDROZOLINE HYDROCHLORIDE agonist
- METHYLDOPATE HYDROCHLORIDE agonist
- GUANFACINE HYDROCHLORIDE agonist
- GUANABENZ ACETATE agonist
- HYDROXYAMPHETAMINE HYDROBROMIDE agonist
- PHENOXYBENZAMINE HYDROCHLORIDE antagonist
- OXYMETAZOLINE HYDROCHLORIDE agonist
- DIPIVEFRIN HYDROCHLORIDE agonist
- PHENTOLAMINE MESYLATE antagonist
- FIPAMEZOLE antagonist
- XYLOMETAZOLINE HYDROCHLORIDE agonist
- EPINEPHRINE BITARTRATE agonist
- CLONIDINE agonist
- NOREPINEPHRINE BITARTRATE agonist
- EPHEDRINE SULFATE agonist
- MOXISYLYTE antagonist
- TOLAZOLINE HYDROCHLORIDE antagonist
- CLONIDINE HYDROCHLORIDE agonist
- NAPHAZOLINE HYDROCHLORIDE agonist
- LOFEXIDINE HYDROCHLORIDE agonist
- AVIPTADIL antagonist
- DROXIDOPA agonist
- DEXMEDETOMIDINE HYDROCHLORIDE agonist
- FADOLMIDINE HYDROCHLORIDE agonist
- ESMIRTAZAPINE MALEATE antagonist
- EPHEDRINE HYDROCHLORIDE agonist
- ERGOLOID MESYLATES antagonist
- ERGOTAMINE TARTRATE agonist
- CELIPROLOL antagonist
- MEPHENTERMINE SULFATE agonist
- ORM-12741 antagonist
- METHYLDOPA agonist
- MIRTAZAPINE antagonist
- LEVONORDEFRIN agonist
- EPINEPHRINE agonist
Related proteins · sequence + function similarity
- Alpha-2C adrenergic receptor 0.99
- Alpha-2C adrenergic receptor 0.99
- Alpha-2C adrenergic receptor 0.99
- Beta-1 adrenergic receptor 0.94
- Beta-1 adrenergic receptor 0.94
- Beta-1 adrenergic receptor 0.94
- Beta-1 adrenergic receptor 0.94
- Alpha-1D adrenergic receptor 0.93
- Beta-1 adrenergic receptor 0.93
- Alpha-1D adrenergic receptor 0.93
- Beta-1 adrenergic receptor 0.93
- Beta-1 adrenergic receptor 0.93
Co-cited proteins · studied together in the literature
- Alpha-2A adrenergic receptor 1 shared papers
Literature · 5 cited papers
- Polymorphisms of cardiac presynaptic alpha2C adrenergic receptors: Diverse intragenic variability with haplotype-specific functional effects. Proc. Natl. Acad. Sci. U.S.A. · 2004
- A four amino acid deletion polymorphism in the third intracellular loop of the human alpha 2C-adrenergic receptor confers impaired coupling to multiple effectors. J. Biol. Chem. · 2000
- Molecular cloning, sequencing and functional study of the promoter region of the human alpha2C4-adrenergic receptor gene. Biochem. J. · 1997
- Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype. Proc. Natl. Acad. Sci. U.S.A. · 1988
- Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR. FEBS Lett. · 1991