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 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 I22 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.

Diagnostics with Modern Chemical Probes

Generation of functional probes by modern chemistry such as CH activation for modified tryptophan peptides and the preparation of fluorescent…

+ info

Neurodegeneration in ageing and neurodegenerative diseases

  We focus our research in the study of the molecular mechanisms involved in behavioral abnormalities and cognitive decline, by using…

+ info

Design, synthesis and evaluation of new polycyclic inhibitors of the M2 channel of the influenza A virus.

Amantadine and rimantadine have been in clinical use as anti-influenza A virus agents for decades. The mechanism of action of…

+ info

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