A series of 4‐aminomethyl‐1,2,3,4‐tetrahydroisoquinoline derivatives were prepared as potential CNS‐agents acting via amino‐acid neurotransmitter systems. The compounds were synthesized from 1,2,3,4‐tetra‐hydro‐1‐oxoisoquinoline‐4‐carboxylic acids obtained by dipolar cycloaddition reactions of imines with homo‐phthalic anhydride. Among the compounds tested 5c and 5m showed sub‐micromolar affinity for the NMDA receptor and represent a structurally novel class of ligand for this site.
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Bonnaud et al. (1993) studied this question.
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