Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 2

Abstract Herein is described a new class of selective σ 1 ligands consisting of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Compound 1a has high affinity (IC 50  = 16 nM) for σ 1 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 (IC 50  ≈ 2–3 nM).