Alpha-2A adrenergic receptor

The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the is_associated_with::human genome encoding it.

Receptor
α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating is_associated_with::neurotransmitter release from is_associated_with::sympathetic nerves and from adrenergic neurons in the is_associated_with::central nervous system. Studies in mice revealed that both the α2A and α2C subtypes were required for normal is_associated_with::presynaptic control of transmitter release from sympathetic nerves in the is_associated_with::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.

Gene
This gene encodes α2A subtype and it contains no is_associated_with::introns in either its coding or is_associated_with::untranslated sequences.

Role in central nervous system
Although the pre-synaptic functions of α2A receptors have been a major focus (see above), the majority of α2 receptors in the brain are actually localized post-synaptically to noradrenergic terminals, and therefore aid in the function of is_associated_with::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.

Agonists

 * is_associated_with::Clonidine
 * is_associated_with::Lofexidine
 * is_associated_with::Dexmedetomidine
 * is_associated_with::Guanfacine

Antagonists

 * is_associated_with::Asenapine
 * is_associated_with::BRL-44408
 * is_associated_with::Clozapine
 * is_associated_with::Lurasidone
 * is_associated_with::Mianserin
 * is_associated_with::Mirtazapine
 * is_associated_with::Paliperidone
 * is_associated_with::Risperidone
 * is_associated_with::Yohimbine