Insights into the Pharmacokinetics and In Vitro Cell-Based Studies of the Imidazoline I₂ Receptor Ligand B06.

ABSTRACT: The impact of neurodegenerative diseases (ND) is becoming unbearable for humankind due to their vast prevalence and the lack of efficacious treatments. In this scenario, we focused on imidazoline I₂ receptors (I₂-IR) that are widely distributed in the brain and are altered in patients with brain disorders. We took the challenge of modulating I₂-IR by developing structurally new molecules, in particular, a family of bicyclic α-iminophosphonates, endowed with high affinity and selectivity to these receptors. Treatment of two murine models, one for age-related cognitive decline and the other for Alzheimer's disease (AD), with representative compound B06 ameliorated their cognitive impairment and improved their behavioural condition. Furthermore, B06<

SUBMITTER: Bagan A 

PROVIDER: S-EPMC9141032 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature