醉椒素

• 常用名: 醉椒素
• 英文名: Kavain
• CAS号: 3155-48-4
• 分子量: 230.259
• 密度: 1.2±0.1 g/cm3
• 沸点: 432.6±45.0 °C at 760 mmHg
• 分子式: C₁₄H₁₄O₃
• 熔点: 142-148ºC
• 闪点: 184.6±23.3 °C
• 符号: GHS07
• 信号词: Warning

醉椒素用途

Kavain是一类从 Piper methysticum 中分离出来的卡瓦酸内酯,对动物和人类具有抗焦虑和镇静作用。Kavain 可以正调控 GABAA 受体。

醉椒素名称

• 中文名: DL-醉椒素
• 英文名: Kavain
• 中文别名: 醉椒素

醉椒素生物活性

• 描述: Kavain是一类从 Piper methysticum 中分离出来的卡瓦酸内酯,对动物和人类具有抗焦虑和镇静作用。Kavain 可以正调控 GABAA 受体。
• 体外研究: 双电极电压钳技术用于表征主要抗焦虑kavalactone,Kavain在人重组α1β2,β2γ2L,αxβ2γ2L,α1βxγ2L和α4β2δγ-氨基丁酸A型受体(GABAARs)中的功能特性。非洲爪蟾卵母细胞。无论亚基组成如何,Kavain都能正向调节所有受体,但α4β2δ的增强程度大于α1β2γ2LGABAARs。KKAAVAIN的调节作用不受氟马西尼的影响,表明Kavain不通过经典的苯二氮卓结合位点增强GABAAR。先前已显示β3N265M点突变显着降低麻醉敏感性,也减少了Kavain介导的增强作用[1]。
• 参考文献:

  [1]. Chua HC, et al. Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism. PLoS One. 2016 Jun 22;11(6):e0157700.

醉椒素物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 432.6±45.0 °C at 760 mmHg
• 熔点: 142-148ºC
• 分子式: C₁₄H₁₄O₃
• 分子量: 230.259
• 闪点: 184.6±23.3 °C
• 精确质量: 230.094299
• PSA: 35.53000
• LogP: 1.69
• InChIKey: XEAQIWGXBXCYFX-BQYQJAHWSA-N
• SMILES: COC1=CC(=O)OC(C=Cc2ccccc2)C1
• 蒸汽压: 0.0±1.0 mmHg at 25°C
• 折射率: 1.565

醉椒素安全信息

• 符号: GHS07
• 信号词: Warning
• 危害声明: H302
• 个人防护装备: dust mask type N95 (US);Eyeshields;Gloves
• 危害码 (欧洲): Xn:Harmful;
• 风险声明 (欧洲): R22
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 3

醉椒素靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro... 来源：NCGC 靶标：N/A External Id：SERCaMPGLuc-p1-antagonist

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：USP8 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 8 External Id：USP8 FAST DUB HTS Primary

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：USP17 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 17 like family member 5 External Id：USP17 FAST DUB HTS Primary

实验名称：USP7 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 7 External Id：USP7 FAST DUB HTS Primary

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

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醉椒素英文别名

• DL-Kawain
• 4-Methoxy-6-[(E)-2-phenylvinyl]-5,6-dihydro-2H-pyran-2-one
• trans-5,6-Dihydro-4-methoxy-6-(2-phenylethenyl)-2H-pyran-2-one,DL-Kawain
• KAVAIN,DL
• UNII:5L1NI60TGB
• Kawain,DL
• Kawain
• Kavain
• MFCD00270446
• DL-KAVAIN