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- W2271796329 abstract "Herein we report the synthesis and biological activity of new sigma receptor (σR) ligands obtained by combining different substituted five-membered heterocyclic rings with appropriate σR pharmacophoric amines. Radioligand binding assay, performed on guinea pig brain membranes, identified 25b (1-(1,4-dioxaspiro[4.5]decan-2-ylmethyl)-4-benzylpiperazine) as the most interesting compound of the series, displaying high affinity and selectivity for σ1R (pKiσ1 = 9.13; σ1/σ2 = 47). The ability of 25b to modulate the analgesic effect of the κ agonist (-)-U-50,488H and μ agonist morphine was evaluated in vivo by radiant heat tail-flick test. It exhibited anti-opioid effects on both κ and μ receptor-mediated analgesia, suggesting an agonistic behavior at σ1R. Docking studies were performed on the theoretical σ1R homology model. The present work represents a new starting point for the design of more potent and selective σ1R ligands." @default.
- W2271796329 created "2016-06-24" @default.
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- W2271796329 date "2016-04-01" @default.
- W2271796329 modified "2023-09-26" @default.
- W2271796329 title "Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives" @default.
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- W2271796329 cites W1992385273 @default.
- W2271796329 cites W1992763610 @default.
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- W2271796329 cites W2003532781 @default.
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- W2271796329 cites W2023202438 @default.
- W2271796329 cites W2025824767 @default.
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- W2271796329 doi "https://doi.org/10.1016/j.ejmech.2016.01.059" @default.
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