The alpha-2C adrenergic receptor (α
2C adrenoceptor), also known as ADRA2C, is an
alpha-2 adrenergic receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-, α2B-, and α2C-adrenergic. Some ...
, and also denotes the human
gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a b ...
encoding it.
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
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell.
Neu ...
release from
sympathetic nerves
The sympathetic nervous system (SNS) is one of the three divisions of the autonomic nervous system, the others being the parasympathetic nervous system and the enteric nervous system. The enteric nervous system is sometimes considered part of the ...
and from adrenergic neurons in the
central nervous system
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all p ...
. 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
The heart is a muscular Organ (biology), organ in most animals. This organ pumps blood through the blood vessels of the circulatory system. The pumped blood carries oxygen and nutrients to the body, while carrying metabolic waste such as ca ...
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.
Gene
This gene encodes the alpha2C subtype, which contains no
introns
An intron is any nucleotide sequence within a gene that is not expressed or operative in the final RNA product. The word ''intron'' is derived from the term ''intragenic region'', i.e. a region inside a gene."The notion of the cistron .e., gene ...
in either its
coding or
untranslated sequences.
Ligands
Agonists
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(R)-3-Nitrobiphenyline
(''R'')-3-Nitrobiphenyline is a drug which acts as an α-adrenergic agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify wha ...
(also weak antagonist at α
2A and α
2B)
Antagonists
*BMY 7378 (also
α1D antagonist)
* JP-1302: selective over α2A, α2B, α2C
* ''N''--2-phenoxy-nicotinamide
*
Quetiapine
Quetiapine, sold under the brand name Seroquel among others, is an atypical antipsychotic medication used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. Despite being widely used as a sleep aid due to its ...
*
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It is taken either by mouth or by injection (subcutaneous or intramuscular). The injectable versions ...
*
Spiroxatrine
Spiroxatrine is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist
A dopamine antagonist, also known as an anti-dopam ...
*
Yohimbine
Yohimbine (), also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe''; also from the bark of the unrelated South American tree ''Aspidosperma quebracho-blanco''. Yohimbine is an α2 ...
derivatives 9 and 10: >43 fold selectivity over α2A, α2B and α1 subtypes
*
Brexpiprazole
Brexpiprazole, sold under the brand name Rexulti among others, is an atypical antipsychotic. It is a dopamine D2 receptor partial agonist and has been described as a "serotonin–dopamine activity modulator" (SDAM). The drug was approved by the ...
See also
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Adrenergic receptor
The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like bet ...
References
External links
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Further reading
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{{G protein-coupled receptors, g1
Adrenergic receptors