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- W3162134450 abstract "σ-1 receptors (σ1R) modulate nociceptive signaling, driving the search for selective antagonists to take advantage of this promising target to treat pain. In this study, a new series of benzylpiperazinyl derivatives has been designed, synthesized, and characterized for their affinities toward σ1R and selectivity over the σ-2 receptor (σ2R). Notably, 3-cyclohexyl-1-{4-[(4-methoxyphenyl)methyl]piperazin-1-yl}propan-1-one (15) showed the highest σ1R receptor affinity (Ki σ1 = 1.6 nM) among the series with a significant improvement of the σ1R selectivity (Ki σ2/Ki σ1 = 886) compared to the lead compound 8 (Ki σ2/Ki σ1 = 432). Compound 15 was further tested in a mouse formalin assay of inflammatory pain and chronic nerve constriction injury (CCI) of neuropathic pain, where it produced dose-dependent (3–60 mg/kg, i.p.) antinociception and anti-allodynic effects. Moreover, compound 15 demonstrated no significant effects in a rotarod assay, suggesting that this σ1R antagonist did not produce sedation or impair locomotor responses. Overall, these results encourage the further development of our benzylpiperazine-based σ1R antagonists as potential therapeutics for chronic pain." @default.
- W3162134450 created "2021-05-24" @default.
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- W3162134450 date "2021-05-21" @default.
- W3162134450 modified "2023-10-04" @default.
- W3162134450 title "Development of New Benzylpiperazine Derivatives as σ<sub>1</sub> Receptor Ligands with <i>in Vivo</i> Antinociceptive and Anti-Allodynic Effects" @default.
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- W3162134450 doi "https://doi.org/10.1021/acschemneuro.1c00106" @default.
- W3162134450 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8291485" @default.
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- W3162134450 hasPublicationYear "2021" @default.
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