Alpha-2C adrenergic receptor

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 release from sympathetic nerves 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

• (R)-3-Nitrobiphenyline (also weak antagonist at α_2A and α_2B)

Antagonists

• BMY 7378 (also α_1D antagonist)
• JP-1302: selective over α2A, α2B, α2C
• spiroxatrine
• yohimbine derivatives 9 and 10: >43 fold selectivity over α2A, α2B and α1 subtypes
• N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide
• Risperidone

See also

• Adrenergic receptor