Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379407 | 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 3a has high affinity (IC50 = 16 nM) for the σ1 receptor and is selective in a large panel of therapeutic targets. This first study presents structural changes around the Tic-hydantoin core, leading to a Tic-hydantoin analogue with a higher σ1 affinity (IC50 ≈ 1 nM).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Julie Charton, Amaury Cazenave Gassiot, Sophie Girault-Mizzi, Marie-Ange Debreu-Fontaine, Patricia Melnyk, Christian Sergheraert,