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Agonist responses of (R)- and (S)-3-fluoro-γ-aminobutyric acids suggest an enantiomeric fold for GABA binding to GABAC receptors

机译:(R)-和(S)-3-氟代-γ-氨基丁酸的激动剂反应表明GABA与GABAC受体结合的对映体折叠

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摘要

The enantiomers of 3F-GABA were evaluated on GABA_C receptors. Both enantiomers were agonists, with the (R)-enantiomer being an order of magnitude more potent. This result is consistent with a folded binding mode for GABA, a conclusion which suggests a different binding mode to that found in the related but pharmacologically distinct GABA_A receptors.
机译:在GABA_C受体上评估了3F-GABA的对映异构体。两种对映体都是激动剂,(R)-对映体更有效。该结果与GABA的折叠结合模式一致,该结论表明与相关但在药理学上不同的GABA_A受体中发现的结合模式不同。

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  • 来源
    《Chemical Communications》 |2011年第28期|p.7956-7958|共3页
  • 作者单位

    Faculty of Pharmacy, University of Sydney, NSW, 2006, Australia;

    University of St Andrews, EASTChem School of Chemistry and Centre for Biomolecular Sciences, North Haugh, St Andrews, Fife,KY16 9ST, UK;

    Faculty of Pharmacy, University of Sydney, NSW, 2006, Australia;

    Faculty of Pharmacy, University of Sydney, NSW, 2006, Australia;

    Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology D06, University of Sydney, NSW, 2006, Australia;

    University of St Andrews, EASTChem School of Chemistry and Centre for Biomolecular Sciences, North Haugh, St Andrews, Fife,KY16 9ST, UK;

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  • 入库时间 2022-08-17 13:22:37

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