I1

Three imidazoline receptor subtypes (I1, I2, and I3) have been proposed and the understanding of each has seen differing progress over the decades. I1 receptors partially mediate the central hypotensive effects of clonidine-like drugs. I2 receptors associate with several distinct proteins, but the identities of these proteins remain elusive. The understanding of I3 receptors is relatively limited. Existing data suggest that I3 receptors may represent a binding site at the Kir6.2-subtype ATP-sensitive potassium channels in pancreatic β-cells and may be involved in insulin secretion. Despite the elusive nature of their molecular identities, recent progress on drug discovery targeting imidazoline receptors (I1 and I2) demonstrates the exciting potential of these compounds to elicit neuroprotection and to treat various disorders such as hypertension, metabolic syndrome, and chronic pain.[1]


[1] P. Bousquet et al. Imidazoline Receptor System: The Past, the Present, and the Future. Pharmacol Rev. 2020 Jan;72(1):50-79.

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3017 BRD4780 Potent and selective imidazoline1 (I1) receptor ligand; TMED9 binder  Recently added €95.00

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