Title :

Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands

Author(s) :

Donnier-Marechal, Marion [Auteur]
Carato, Pascal [Auteur]
Le Broc-Ryckewaert, Delphine [Auteur]
Furman, Christophe [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center (LIRIC) - U995
Melnyk, Patricia [Auteur]

Lille Neurosciences & Cognition (LilNCog) - U 1172

Journal title :

European journal of medicinal chemistry

Abbreviated title :

Eur. J. Med. Chem.

Volume number :

92

Pages :

575-582

Publication date :

2015-03-06

ISSN :

0223-5234

English keyword(s) :

Sigma 1
Benzimidazolone
Benzimidazole
Benzazolinone
Alzheimer

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

The σ1 proteins are considered to be a new class of target structures for several central nervous system disorders, including depression, anxiety, psychosis, and Parkinson's and Alzheimer's diseases. Recently, the involvement ...
Show more >The σ1 proteins are considered to be a new class of target structures for several central nervous system disorders, including depression, anxiety, psychosis, and Parkinson's and Alzheimer's diseases. Recently, the involvement of these receptors in neuropathic pain and cancer has also been observed. So far, only a few ligands are in clinical trials. In a continuation of our previous studies on the development of σ1 ligands, a new series of benzannulated heterocycles was designed and synthesised. In vitro competition binding assays showed that many of them possessed high σ1 receptor affinity (Ki = 0.6-10.3 nM), and good σ2/σ1 subtype selectivity, without cytotoxic effects on SY5Y cells (human neuroblastoma cell line).Show less >

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
• Lille Neurosciences & Cognition (LilNCog) - U 1172

Research team(s) :

Therapeutic innovation targetting inflammation

Submission date :

2019-05-17T13:14:34Z