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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 I2A (amiloride-sensitive) and I2B (amiloride-insensitive). A putative I3 has been described which enhances insulin secretion.
Imidazoline Receptor Target Files
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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 | I1 | I2 | I3 |
|---|
| Location | Lateral reticular nucleus, locus ceruleus, kidney, platelets, pancreas | Interpeduncular and arcuate nuclei, pineal gland, liver, kidney, heart, striated muscle, MAO | Pancreatic β cells |
| Transduction Mechanism | ↑ Diacylglycerol and arachidonic acid | Unknown | Unknown |
| Key Selective Ligands |
AGN 192403 (1072) Clonidine (0690) Rilmenidine (0790) |
BU 239 (0726) RS 45041-190 (0889) 2-BFI (0348) |
KU14R (1131) |
| Putative Endogenous Ligands | Agmatine (0842), Harmane (1132) | ||
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