Title of article :
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 1
Author/Authors :
Julie Charton، نويسنده , , Amaury Cazenave Gassiot، نويسنده , , Sophie Girault-Mizzi، نويسنده , , Marie-Ange Debreu-Fontaine، نويسنده , , Patricia Melnyk، نويسنده , , Christian Sergheraert، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
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).
Keywords :
Hydantoin , TiC , Selectivity , ? receptors
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters