Methylation of imidazoline related compounds leads to loss of alpha(2)-adrenoceptor affinity. Synthesis and biological evaluation of selective I(1) imidazoline receptor ligands.

Date publication

août 2012

Auteurs

Membres identifiés du Cancéropôle Est :
Dr DONTENWILL Monique , Dr BRUBAN Véronique

Tous les auteurs :
Schann S, Greney H, Gasparik V, Dontenwill M, Rascente C, Lacroix G, Monassier L, Bruban V, Feldman J, Ehrhardt JD, Bousquet P

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/22750139

Résumé

Methylated analogues of imidazoline related compounds (IRC) were prepared; their abilities to bind I(1) imidazoline receptors (I(1)Rs), I(2) imidazoline binding sites (I(2)BS) and alpha(2)-adrenoceptor subtypes (alpha(2)ARs) were assessed. Methylation of the heterocyclic moiety of IRC resulted in a significant loss of alpha(2)AR affinity. Amongst the selective ligands obtained, LNP 630 (4) constitutes the first highly selective I(1)R agent showing hypotensive activity after intravenous administration.

Référence

Bioorg Med Chem. 2012 Aug 1;20(15):4710-5