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  • Title: Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
    Author: Cazenave Gassiot A, Charton J, Girault-Mizzi S, Gilleron P, Debreu-Fontaine MA, Sergheraert C, Melnyk P.
    Journal: Bioorg Med Chem Lett; 2005 Nov 01; 15(21):4828-32. PubMed ID: 16140009.
    Abstract:
    Herein is described a new class of selective sigma1 ligands consisting of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Compound 1a has high affinity (IC50 = 16 nM) for sigma1 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 approximately 2-3 nM).
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