The imidazoline I2 receptors (I2-IRs) are altered in the brain of Alzheimer’s disease patients and I2-IR ligands may have therapeutic potential as neuroprotective agents. Since structural data for I2-IR remains unknown, the discovery of selective I2-IR ligands is likely to provide valuable tools in defining the pharmacological characterization of these receptors.
We are interested in the pharmacological characterization of a new family of (2-imidazolin-4-yl)phosphonates that displayed high affinity for I2-IRs, and high I2/α2 selectivity. In vivo studies in the female SAMP8 mice showed that treatments with two of our previously reported I2-IR ligands produce beneficial effects in behavior and cognition.
Changes in molecular pathways demonstrate the neuroprotective role for these new I2-IR ligands, being promising therapeutic agents in brain disorders and age-related neurodegenerative diseases.
New imidazoline I2 receptor ligands


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New imidazoline I2 receptor ligands
The imidazoline I2 receptors (I2-IRs) are altered in the brain of Alzheimer’s disease patients and I2-IR ligands may have therapeutic…
+ info