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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Minimal structural requirements of alkyl gamma-lactones capable of antagonizing the cocaine-induced motility decrease in planarians.
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Minimal structural requirements of alkyl gamma-lactones capable of antagonizing the cocaine-induced motility decrease in planarians.

机译：能够对抗可卡因诱导的运动的烷基γ-内酯的最低结构要求在涡虫中降低。

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摘要

We recently reported that the natural cyclic lactone, parthenolide, and related analogs prevent the expression of behavioral effects induced by cocaine in planarians and that parthenolide's gamma-lactone ring is required for this effect. In the present work, we tested a series of alkyl gamma-lactones with varying chain length (1-8 carbons) to determine their ability to antagonize the planarian motility decrease induced by 200 muM cocaine. Alkyl lactones with up to a 4-carbon alkyl chain did not affect planarian motility or antagonized the cocaine-induced motility decrease; only the compound gamma-nonalactone (a gamma-lactone with a 5-carbon chain) was able to prevent the cocaine-induced behavioral patterns, while alkyl lactones with longer carbon chains failed to prevent the cocaine-induced effects. Thus, we conclude that the optimal structural features of this family of compounds to antagonize cocaine's effect in this experimental system is a gamma-lactone ring with at a 5-carbon long functional group.
机译：我们最近报道，天然环内酯，单烯菊酯及相关类似物可防止可卡因在刨刀中表达行为效应，而该效应需要单烯酚的γ-内酯环。在目前的工作中，我们测试了一系列具有不同链长（1-8个碳原子）的烷基γ-内酯，以确定它们拮抗200μM可卡因引起的涡虫运动性降低的能力。具有最多4个碳烷基链的烷基内酯不影响涡虫运动性或拮抗可卡因引起的运动性下降;只有化合物γ-非内酯（具有5个碳链的γ-内酯）能够阻止可卡因诱导的行为模式，而具有较长碳链的烷基内酯则不能阻止可卡因诱导的行为。因此，我们得出结论，在该实验系统中拮抗可卡因作用的该化合物家族的最佳结构特征是具有5个碳原子长的官能团的γ-内酯环。

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