Titre :

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

Auteur(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

Titre de la revue :

European journal of medicinal chemistry

Nom court de la revue :

Eur. J. Med. Chem.

Numéro :

92

Pagination :

575-582

Date de publication :

2015-03-06

ISSN :

0223-5234

Mot(s)-clé(s) en anglais :

Sigma 1
Benzimidazolone
Benzimidazole
Benzazolinone
Alzheimer

Discipline(s) HAL :

Sciences du Vivant [q-bio]

Résumé en anglais : [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 ...
Lire la suite >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).Lire moins >

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

CHU Lille
Inserm
Université de Lille

Collections :

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

Équipe(s) de recherche :

Therapeutic innovation targetting inflammation

Date de dépôt :

2019-05-17T13:14:34Z