Gidazepam

• 常用名: Gidazepam
• 英文名: Gidazepam
• CAS号: 129186-29-4
• 分子量: 387.23100
• 密度: 1.58g/cm3
• 沸点: 675.6ºC at 760mmHg
• 分子式: C₁₇H₁₅BrN₄O₂
• 熔点: N/A
• 闪点: 362.4ºC

Gidazepam用途

Gidazepam 是一种 GABA 受体通道 (GABA RCs) 激动剂。

Gidazepam名称

• 中文名: Gidazepam
• 英文名: 2-(7-bromo-2-oxo-5-phenyl-3H-1,4-benzodiazepin-1-yl)acetohydrazide

Gidazepam生物活性

• 描述: Gidazepam 是一种 GABA 受体通道 (GABA RCs) 激动剂。
• 相关类别:
  信号通路 >> 跨膜转运 >> GABA受体
  信号通路 >> 神经信号通路 >> GABA受体
  研究领域 >> 神经疾病
• 靶点实验:

  GABA receptor[1]

• 体外研究: Gidazepam对GABA RCs的亲和力显着低于phenazepam,3- hydrozyphenazepam和Br-nordiazepam。这表现为苯并二氮杂受体特异性配体地西泮结合的抑制常数(Ki)的不同值。对于Gidazepam,Ki值为2,200±50 nM [1]。
• 体内研究: 将小鼠分成10组,每组5只,用Gidazepam(GDZ,1mg/kg)口服治疗;酯1(175mg/kg);酯2(20mg/kg);酯3和4(200毫克/千克); Gidazepam和酯1-4的混合物。所有GABA与单萜的酯在口服给药后3小时显示抗癫痫作用,如通过诱导阵挛-强直性惊厥(DCTC)和强直延长(DTE)值的增加所证明的。发现Gidazepam(1 mg/kg)可以防止癫痫发作,DCTC和DTE值分别为250％和215％;与单独使用每种化合物相比,联合给予Gidazepam和5-7酯可显着增加抗惊厥活性[1]。
• 动物实验: 小鼠[1]使用杂交的雄性白色小鼠（18-22g）。将小鼠分成10组，每组5只，用Gidazepam 1mg / kg（GDZ）口服治疗;薄荷醇的GABA酯175 mg / kg（1）;百里香酚GABA酯20 mg / kg（2）;香芹酚的GABA酯200mg / kg（3）;愈创木酚的GABA酯200mg / kg（4）; Gidazepam和1的混合物; Gidazepam和2的混合物; Gidazepam和3的混合物;基于我们的初步研究和文献引用，相对于单萜以酯的等摩尔量计算酯G的剂量1-4的混合物。在急性全身性癫痫发作的模型中评价化合物1-4和吉西他嗪以及吉西他嗪与1-4的混合物的抗惊厥活性。化合物的药理作用估计在3小时内[1]。
• 参考文献:

  [1]. N. Ya Golovenko, et al. Pharmacodynamical and Neuroreceptor Analysis of the Permeability of the Blood-Brain Barrier for Derivatives of 1,4-Benzodiazepine. Neurophysiology, Vol. 46, No. 3, June, 2014.

  [2]. Nesterkina M, et al. Synthesis and Pharmacological Properties of Novel Esters Based on Monocyclic Terpenes and GABA. Pharmaceuticals (Basel). 2016 Jun 13;9(2). pii: E32.

Gidazepam物理化学性质

• 密度: 1.58g/cm3
• 沸点: 675.6ºC at 760mmHg
• 分子式: C₁₇H₁₅BrN₄O₂
• 分子量: 387.23100
• 闪点: 362.4ºC
• 精确质量: 386.03800
• PSA: 91.28000
• LogP: 2.66420
• InChIKey: XLGCMZLSEXRBSG-UHFFFAOYSA-N
• SMILES: NNC(=O)CN1C(=O)CN=C(c2ccccc2)c2cc(Br)ccc21
• 蒸汽压: 4.14E-18mmHg at 25°C
• 折射率: 1.698
• 储存条件: 2-8℃

Gidazepam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：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：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：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.

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

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Gidazepam英文别名

• (1-Hydrazinocarbonyl)-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one
• UNII-XMJ87I93Y9
• 1H-1,4-Benzodiazepine-1-aceticacid,7-bromo-2,3-dihydro-2-oxo-5-phenyl-,hydrazide
• gidazepam