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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 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.
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.
Tocris offers the following scientific literature for Imidazoline Receptors to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Our new product guide highlights over 215 new products added to the Tocris Bioscience range during the first half of 2019.
|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)
BU 239 (0726)
RS 45041-190 (0889)
|Putative Endogenous Ligands||Agmatine (0842), Harmane (1132)|