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  • Title: Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
    Author: Charton J, Cazenave Gassiot A, Girault-Mizzi S, Debreu-Fontaine MA, Melnyk P, Sergheraert C.
    Journal: Bioorg Med Chem Lett; 2005 Nov 01; 15(21):4833-7. PubMed ID: 16140011.
    Abstract:
    Herein is described a new class of selective sigma1 ligands consisting of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Compound 3a has high affinity (IC50 = 16 nM) for the sigma1 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 sigma1 affinity (IC50 approximately 1 nM).
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