Title of article
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 2
Author/Authors
Amaury Cazenave Gassiot، نويسنده , , Julie Charton، نويسنده , , Sophie Girault-Mizzi، نويسنده , , Pauline Gilleron، نويسنده , , Marie-Ange Debreu-Fontaine، نويسنده , , Christian Sergheraert، نويسنده , , Patricia Melnyk، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
4828
To page
4832
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).
Keywords
Hydantoin , ?-Receptors , Selectivity , TiC
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796085
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