Alpha-2A adrenergic receptor

Alpha-2A adrenergic receptor (ADRA2A) is a type of adrenergic receptor that is encoded by the ADRA2A gene in humans. It is a G protein-coupled receptor (GPCR) associated with the Gi/Go alpha subunit and is expressed in various tissues and cells, including the central nervous system, blood vessels, and fat cells.

Function

The Alpha-2A adrenergic receptor plays a crucial role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. This receptor is responsible for the presynaptic inhibition of norepinephrine release, which reduces the rate of firing of the postganglionic sympathetic nerves. It also mediates the central control of blood pressure, thermoregulation, and sedation.

Clinical significance

Alterations in the function or expression of the Alpha-2A adrenergic receptor have been implicated in various diseases and disorders. For instance, polymorphisms in the ADRA2A gene have been associated with an increased risk of type 2 diabetes and hypertension. Moreover, the receptor is a target for various drugs used in the treatment of hypertension, psychiatric disorders, and pain.

Pharmacology

The Alpha-2A adrenergic receptor is a target for several classes of drugs, including alpha-2 adrenergic agonists and alpha-2 adrenergic antagonists. Agonists such as clonidine and dexmedetomidine are used in the treatment of hypertension and sedation, respectively. Antagonists such as yohimbine and atipamezole are used in the treatment of erectile dysfunction and reversal of sedation, respectively.

See also

• Alpha-2 adrenergic receptor
• Adrenergic receptor
• G protein-coupled receptor
• Neurotransmitter