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Sigma Receptor Binding Profile of a Series of Analgesic Tropane Derivatives

The binding profile on sigma receptor subtypes of a family of tropane derivatives, previously studied as analgesic and nootropic drugs, is reported. The results show that the sigma receptors are not involved in the enhancement of acetylcholine release and of the consequent analgesic activity of this class of drugs. Structure‐affinity relationships for σ receptor subtypes are discussed.They lead to the identification of a few useful leads for further development of potent sigma ligands within the series.