The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the human gene encoding it.[4]
α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mice revealed that both the α2A and α2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the α2A subtype inhibited transmitter release at high stimulation frequencies, whereas the α2C subtype modulated neurotransmission at lower levels of nerve activity[5]
Gene[]
This gene encodes α2A subtype and it contains no introns in either its coding or untranslated sequences.[4]
Role in central nervous system[]
Although the pre-synaptic functions of α2A receptors are often a major focus, the majority of α2 receptors in the brain are actually localized post-synaptically to noradrenergic terminals[citation needed], and therefore aid in the function of norepinephrine. Many post-synaptic α2A receptors have important effects on brain function; for example, α2A receptors are localized on prefrontal cortical neurons where they regulate higher cognitive function[citation needed].
^Hein, Lutz; Altman, John D.; Kobilka, Brian K. (1999). "Two functionally distinct α2-adrenergic receptors regulate sympathetic neurotransmission". Nature. 402 (6758): 181–184. Bibcode:1999Natur.402..181H. doi:10.1038/46040. PMID10647009. S2CID205047992.
External links[]
"α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Human ADRA2A genome location and ADRA2A gene details page in the UCSC Genome Browser.
Human ZNF32 genome location and ZNF32 gene details page in the UCSC Genome Browser.
Further reading[]
Perälä M, Hirvonen H, Kalimo H, Ala-Uotila S, Regan JW, Akerman KE, Scheinin M (Nov 1992). "Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues". Brain Research. Molecular Brain Research. 16 (1–2): 57–63. doi:10.1016/0169-328X(92)90193-F. PMID1334200.
Surprenant A, Horstman DA, Akbarali H, Limbird LE (Aug 1992). "A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents". Science. 257 (5072): 977–80. Bibcode:1992Sci...257..977S. doi:10.1126/science.1354394. PMID1354394.
Wang CD, Buck MA, Fraser CM (Aug 1991). "Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): 168–79. PMID1678850.
Shilo L, Sakaue M, Thomas JM, Philip M, Hoffman BB (Jan 1994). "Enhanced transcription of the human alpha 2A-adrenergic receptor gene by cAMP: evidence for multiple cAMP responsive sequences in the promoter region of this gene". Cellular Signalling. 6 (1): 73–82. doi:10.1016/0898-6568(94)90062-0. PMID8011430.