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.
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.
Neuro ...
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. 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.
Gene
This gene encodes the alpha2C subtype, which contains no
introns 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, selective for the α subtype, as well as being a weak antagonist at the α and α subtypes. It has been used in scientific research to characterize the binding an ...
(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
*
Risperidone
*
Spiroxatrine
*
Yohimbine 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 th ...
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 beta ...
References
External links
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Further reading
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{{G protein-coupled receptors, g1
Adrenergic receptors