I am a
Home I AM A Search Login

Papers of the Week

Papers: 11 Feb 2023 - 17 Feb 2023

Basic Science

Animal Studies, Pharmacology/Drug Development

Neuropathic Pain

2023 Jan 19

Int J Mol Sci




Design, Synthesis and Pharmacological Evaluation of New Quinoline-Based Panx-1 Channel Blockers.


Crocetti L, Giovannoni MP, Guerrini G, Lamanna S, Melani F, Bartolucci G, Pallecchi M, Paoli P, Lippi M, Wang J, Dahl G


Pannexins are an interesting new target in medicinal chemistry, as they are involved in many pathologies such as epilepsy, ischemic stroke, cancer and Parkinson’s disease, as well as in neuropathic pain. They are a family of membrane channel proteins consisting of three members, Panx-1, Panx-2 and Panx-3, and are expressed in vertebrates. In the present study, as a continuation of our research in this field, we report the design, synthesis and pharmacological evaluation of new quinoline-based Panx-1 blockers. The most relevant compounds and show an IC = 3 and 1.5 µM, respectively, and are selective Panx-1 blockers. Finally, chemical stability, molecular modelling and X-ray crystallography studies have been performed providing useful information for the realization of the project.