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 alpha subunit, Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-adrenergic, α2A-, ...
, and also denotes the human
gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...
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 Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell.
Neurotra ...
release from
sympathetic nerves
The sympathetic nervous system (SNS or SANS, sympathetic autonomic nervous system, to differentiate it from the somatic nervous system) is one of the three divisions of the autonomic nervous system, the others being the parasympathetic nervous sy ...
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, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity o ...
. Studies in mice revealed that both the alpha
2A and alpha
2C subtypes were required for normal
presynaptic
In the nervous system, a synapse is a structure that allows a neuron (or nerve cell) to pass an electrical or chemical signal to another neuron or a target effector cell. Synapses can be classified as either chemical or electrical, depending o ...
control of transmitter release from sympathetic nerves in the
heart
The heart is a muscular Organ (biology), organ found in humans and other animals. This organ pumps blood through the blood vessels. The heart and blood vessels together make the circulatory system. The pumped blood carries oxygen and nutrie ...
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 Nucleic acid sequence, 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 ...
in either its
coding or
untranslated sequences.
Ligands
Agonists
*
(R)-3-Nitrobiphenyline (also weak antagonist at α
2A and α
2B)
Antagonists
* BMY 7378 (also
α1D antagonist)
*
Brexpiprazole
Brexpiprazole, sold under the brand name Rexulti among others, is an atypical antipsychotic medication used for the treatment of major depressive disorder, schizophrenia, and Agitation (dementia), agitation associated with dementia due to Alzhe ...
* JP-1302: selective over α2A, α2B, α2C
* ''N''--2-phenoxy-nicotinamide
*
Pirepemat
Pirepemat (; developmental code name IRL752 or IRL-752) is a drug which is under development for the prevention of falls in people with Parkinson's disease and Parkinson's disease dementia. It has been referred to as a " nootrope" (i.e., nootro ...
*
Quetiapine
Quetiapine ( ), sold under the brand name Seroquel among others, is an atypical antipsychotic medication used in the treatment of schizophrenia, bipolar disorder, bipolar depression, and major depressive disorder. Despite being widely prescri ...
*
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder, as well as aggressive and self-injurious behaviors associated with autism spectrum disorder. It is t ...
*
Mirtazapine
Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to four weeks but ca ...
*
Spiroxatrine
Spiroxatrine (Spiroxamide, R5188) 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 effects and a relatively weak opio ...
*
Yohimbine
Yohimbine, also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe'' (yohimbe); also from the bark of the unrelated South American tree '' Aspidosperma quebracho-blanco''. Yohimbine is ...
derivatives 9 and 10: >43 fold selectivity over α2A, α2B and α1 subtypes
See also
*
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 b ...
References
External links
*
Further reading
*
*
*
*
*
*
*
*
*
*
*
*
*
*
*
*
*
*
*
*
{{G protein-coupled receptors, g1
Adrenergic receptors