Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379406 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
Herein is described a new class of selective σ1 ligands consisting of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Compound 1a has high affinity (IC50 = 16 nM) for σ1 receptor and is selective in a large panel of therapeutic targets. This study presents structural changes on the side chain of the Tic-hydantoin core. Analogs of higher affinity could be identified (IC50 ≈ 2–3 nM).
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Amaury Cazenave Gassiot, Julie Charton, Sophie Girault-Mizzi, Pauline Gilleron, Marie-Ange Debreu-Fontaine, Christian Sergheraert, Patricia Melnyk,