Adrenergic alpha-2 Receptor Agonists Small Molecules and Peptides

Adrenergic α₂ receptors (α₂-adrenoceptors) are members of the adrenergic receptor group of G-protein-coupled receptors that also includes α_1A, α_1B, α_1D, β₁, β₂ and β₃. Adrenergic α₂ receptors are divided into three subtypes: α_2A, α_2B and α_2C, which are widely distributed in both the CNS and periphery. α₂-adrenoceptors play a role in the modulation of neurotransmission, smooth muscle contraction and thermoregulation. A fourth pharmacological subtype, α_2D, has been identified in the rat which is thought to be a species ortholog of the human α_2A subtype.