Imidazoline Receptors

Imidazoline binding sites were originally classified into I₁ sites (labeled by clonidine) and I₂ sites (labeled by idazoxan). I₂ sites have been further classified into I_2A (amiloride-sensitive) and I_2B (amiloride-insensitive). A putative I₃ has been described which enhances insulin secretion. Imidazoline receptors are orphan proteins and their biological function has primarily been established by binding of selective ligands, although their protein identity has yet to be determined.

Targets

Imidazoline Receptor Target Files

Related Targets

Imidazoline receptors have a physiological role in the central regulation of blood pressure. Activation of I₁ receptors decreases sympathetic tone via a central mechanism, which has a hypotensive effect and reduces plasma catecholamine levels. In contrast, I₂-mediated monoamine oxidase inhibition has a hypertensive effect and increases plasma catecholamine levels.

Receptor Data

Properties of Imidazoline Receptors