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Issue 35, 2018, Issue in Progress
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4-Hydroxybenzyl alcohol derivatives and their sedative–hypnotic activities

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Abstract

4-Hydroxybenzyl alcohol (HBA), one of the characteristic active components of Gastrodia elata, exhibits obvious effects on the human central nervous system. In order to acquire compounds with superior bioactivity, 10 derivatives of HBA were synthesized from HBA and carboxylic acids. The sedative effects of the 10 HBA derivatives were evaluated using a spontaneous locomotor activity test (SLT) in mice, and their hypnotic effects were determined to be synergistic with pentobarbital-induced sleep. The results showed that 4-hydroxybenzyl alcohol 3-furancarboxylic acid diester (2FHBA, 10 mg kg−1) exhibited the strongest sedative–hypnotic activity among HBA and its derivatives, and 2FHBA could reverse the insomnia caused by p-chlorophenylalanine (pCPA), flumazenil (FLU) and thiosemicarbazide (TSC). Meanwhile, 2FHBA and 5-hydroxytryptophan (5-HTP) showed a synergistic effect. The results suggested that 2FHBA might be a potential agent against insomnia, which might be mediated by the serotonergic and GABAergic systems.

Graphical abstract: 4-Hydroxybenzyl alcohol derivatives and their sedative–hypnotic activities

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Publication details

The article was received on 06 Mar 2018, accepted on 04 May 2018 and first published on 29 May 2018


Article type: Paper
DOI: 10.1039/C8RA01972J
Citation: RSC Adv., 2018,8, 19539-19550
  • Open access: Creative Commons BY-NC license
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    4-Hydroxybenzyl alcohol derivatives and their sedative–hypnotic activities

    H. Zhu, D. Zhang, Q. Zhang, Y. Zhao, Z. He, Y. Gao and L. Zhang, RSC Adv., 2018, 8, 19539
    DOI: 10.1039/C8RA01972J

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