Introduction of ADRA2C
ADRA2C is one of the three defined subtypes of alpha-2-adrenergic receptors (alpha2A, alpha2B, and alpha2C), which are members of the G protein-coupled receptor family. These receptors regulate a wide range of physiological functions and are targets of clinically important antihypertensive and anesthetic agents. Moreover, they are found to play a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Both mice and human have alpha2C expressed. Alpha2C receptors are present in the basal ganglia, olfactory tubercle, hippocampus, and cerebral cortex. However, alpha2C is the least characterized subtype of adrenergic receptors and still very little is known about the pathophysiological roles of this receptor.
|Basic Information of ADRA2C|
|Protein Name||Alpha-2C adrenergic receptor|
|Aliases||Alpha-2 adrenergic receptor subtype C4, Alpha-2C adrenoreceptor|
|Organism||Homo sapiens (Human)|
Functions of ADRA2C Membrane Protein
Alpha2C appears to be involved in many CNS processes. For instance, it may mediate cold-induced vasoconstriction. Moreover, it can inhibit dopamine release in basal ganglia, as well as serotonin secretion in mouse hippocampal or cerebral cortex slices. Studies involving knockout and transgenic rodents have highlighted some specific functions related to this receptor. Alpha2C-deficient mice show clear-cut behavioral changes, such as increased amphetamine-induced locomotor activity, startle reactivity, aggression, and activity in the forced swim test, while contrary changes are observed in mice with alpha2C overexpression. These results indicate that the alpha2C subtype has a distinct inhibitory role in the processing of sensory information and in the control of motor- and emotion-related activities in the CNS. As a result, this receptor may be of therapeutic value in the treatment of various neuropsychiatric disorders.
Applications of ADRA2C Membrane Protein in Literature
1. Szőllősi E., et al. Cell-based and virtual fragment screening for adrenergic α2C receptor agonists. Bioorganic & Medicinal Chemistry. 2015, 23(14): 3991-3999. PMID: 25648685
This article reported a cell-based high concentration screening and the virtual fragment screening for identification of adrenergic α2C receptor agonists.
2. Carl M. Hurt., et al. Common α2A and α2C adrenergic receptor polymorphisms do not affect plasma membrane trafficking. Naunyn-Schmiedeberg's Archives of Pharmacology. 2014, 387(6): 569-579. PMID: 24643471
This article assessed whether two common human α2A and α2C adrenergic receptor (AR) variants (α2A N251K and α2C Δ322-325 ARs) affected intracellular trafficking or plasma membrane expression.
3. Kurko D., et al. Analysis of functional selectivity through G protein-dependent and-independent signaling pathways at the adrenergic α2C receptor. Brain research bulletin. 2014, 107: 89-101. PMID: 25080296
This article tested a series of agonists targeting the alpha2C receptor and detected the differences in their ability to modulate cAMP accumulation, cytoplasmic Ca2+ release, β-arrestin recruitment, and receptor internalization.
4. Jahnsen J A. and Uhlén S. The C-terminal half of the α2C-adrenoceptor determines the receptor's membrane expression level and drug selectivity. Naunyn-Schmiedeberg's Archives of Pharmacology. 2013, 386(12): 1031-1040. PMID: 23868076
This study investigated which regions of the α2C-adrenoceptor were involved in regulating the expression of binding-competent receptors at the plasma membrane. The results showed that the selectivity mainly resided in the C-terminal half of the receptors.
ADRA2C Preparation Options
Creative Biolabs is a leading service provider in difficult-to-prepare membrane proteins for applications such as immunogen preparation, assays development, and others. With our integrated multiple technologies and the powerful versatile Magic™ membrane protein platform, we are able to provide different formats of functional membrane proteins using various robust reconstitution systems. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-ADRA2C antibody development services.
Depending on the type of mechanistic and functional information you require with the target protein, Creative Biolabs can help you with the appropriate choice of reconstitution strategies and methods. Please feel free to contact us for more information.