Imidazoline 2 (I2) Receptor Ligands Small Molecules and Peptides

Imidazoline 2 receptors (I₂) (labeled by idazoxan) are members of the imidazoline family of receptors, which also include I₁ (labeled by clonidine) and I₃ receptors. I₂ receptors are localized to the mitochondrial membrane and are found in the interpeduncular nucleus, arcuate nucleus, pineal gland, liver, heart, kidney, white adipocytes and striated muscle. Furthermore, I₂ receptors constitute an allosteric binding site of monoamine oxidase (MAO) A and MAO-B.

Little is known about the transduction mechanism of I₂ receptors and the gene encoding it has not yet been characterized. Studies suggest a role for I₂ receptors in Alzheimer's disease, depression and pain.