(-)-双环甲硫脲

• 常用名: (-)-双环甲硫脲
• 英文名: Bicuculline methiodide
• CAS号: 40709-69-1
• 分子量: 509.29
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₀INO₆
• 熔点: N/A
• 闪点: N/A

(-)-双环甲硫脲用途

荷包牡丹甲酰亚胺是一种有效的GABA(a)受体阻滞剂。二瓜氨酸甲酰化物改变膜的性质和燃烧模式。荷包牡丹碱甲酰亚胺降低了Apamin敏感的超极化后,而Apamin是一种从蜂毒中分离出来的毒素,用于阻断小电导Ca2+激活的K+通道。荷包牡丹碱甲碘化物通过阻断apamin敏感的Ca2+激活的K+电流促进突发放电[1]。

(-)-双环甲硫脲名称

• 中文名: (-)-双环甲硫脲
• 英文名: (-)-Bicuculline methiodide,[R-(R*,S*)]-5-(6,8-Dihydro-8-oxofuro[3,4-e]-1,3-benzodioxol-6-yl)-5,6,7,8-tetrahydro-6,6-dimethyl-1,3-dioxolo[4,5-g]isoquinoliniumiodide

(-)-双环甲硫脲生物活性

• 描述: 荷包牡丹甲酰亚胺是一种有效的GABA(a)受体阻滞剂。二瓜氨酸甲酰化物改变膜的性质和燃烧模式。荷包牡丹碱甲酰亚胺降低了Apamin敏感的超极化后,而Apamin是一种从蜂毒中分离出来的毒素,用于阻断小电导Ca2+激活的K+通道。荷包牡丹碱甲碘化物通过阻断apamin敏感的Ca2+激活的K+电流促进突发放电[1]。
• 相关类别:
  信号通路 >> 跨膜转运 >> GABA受体
  研究领域 >> 神经疾病
  信号通路 >> 神经信号通路 >> GABA受体
• 体外研究: 二次甲基二瓜氨酸(30μM)促进 N个-甲基-天-天冬氨酸 (纳米达)刺激,促进多巴胺神经元的爆发性放电[1] 研究表明,反奖励中枢外侧缰核(左b)的簇状放电是抑郁症发生的充分条件。左心室神经元常分为三类：沉默型(无声),强直放电型(补烧)簇状放电型(连发射击)[2]
• 参考文献:

  [1]. Johnson SW, et al. Bicuculline methiodide potentiates NMDA-dependent burst firing in rat dopamine neurons by blocking apamin-sensitive Ca2+-activated K+ currents. Neurosci Lett. 1997 Aug 1;231(1):13-6.

  [2]. Yang Y, et al. Ketamine blocks bursting in the lateral habenula to rapidly relieve depression[J]. Nature, 2018, 554(7692): 317-322.

(-)-双环甲硫脲物理化学性质

• 分子式: C₂₁H₂₀INO₆
• 分子量: 509.29
• 精确质量: 509.03400
• PSA: 63.22000
• InChIKey: HKJKCPKPSSVUHY-GRTNUQQKSA-M
• SMILES: C[N+]1(C)CCc2cc3c(cc2C1C1OC(=O)c2c1ccc1c2OCO1)OCO3.[I-]
• 储存条件: 室温

(-)-双环甲硫脲安全信息

• 个人防护装备: Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
• 危险品运输编码: NONH for all modes of transport

(-)-双环甲硫脲靶点实验

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：Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1315

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：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

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(-)-双环甲硫脲英文别名

• bicuculine methiodide