美喹他嗪

• 常用名: 美喹他嗪
• 英文名: Mequitazine
• CAS号: 29216-28-2
• 分子量: 322.467
• 密度: 1.3±0.1 g/cm3
• 沸点: 469.4±24.0 °C at 760 mmHg
• 分子式: C₂₀H₂₂N₂S
• 熔点: 143-145ºC
• 闪点: 237.7±22.9 °C

美喹他嗪用途

Mequitazine是一种有效的,非依赖性和长效的组胺H1拮抗剂。

美喹他嗪名称

• 中文名: 美喹他嗪
• 英文名: Mequitazine
• 中文别名: 甲喹吩嗪 | 10-(1-氮杂双环[2.2.2]辛烷-3-基甲基)-10H-吩噻嗪

美喹他嗪生物活性

• 描述: Mequitazine是一种有效的,非依赖性和长效的组胺H1拮抗剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
• 体外研究: 美喹他嗪是一种有效的H1受体选择性抗组胺药,被广泛研究并用于过敏性疾病,如花粉症和荨麻疹[1]。美喹他嗪对所有测试的临床分离株(包括Ps)表现出显着的杀菌作用。铜绿假单胞菌。它对革兰氏阳性菌株的作用更明显[2]。
• 体内研究: 美喹他嗪和克立咪唑竞争性地拮抗组胺对豚鼠回肠的作用。在107处的美喹他嗪产生剂量-反应曲线与大鼠十二指肠中的乙酰胆碱的平行移动。最高浓度的美喹他嗪显示出抗胆碱能活性[3]。美喹他嗪抑制大鼠主动脉对KCl,去氧肾上腺素(PE),5-羟色胺(5-HT)和Ca2 +的收缩反应[4]。
• 参考文献:

  [1]. Gonnot V, et al. Expedient synthesis of mequitazine an antihistaminic drug by palladium catalyzed allylic alkylation of sodium phenothiazinate. Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1300-2.

  [2]. El-Nakeeb MA, et a. In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates. Braz J Microbiol. 2011 Jul;42(3):980-91.

  [3]. Martinez-Mir I, et al. Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole. J Pharm Pharmacol. 1988 Sep;40(9):655-6.

  [4]. Satake N, et al. Possible mechanisms of vasoinhibitory effects of mequitazine, an antiallergic agent, on the contractions of isolated rat aorta induced by K+, phenylephrine, 5-hydroxytryptamine, and Ca2+. J Cardiovasc Pharmacol. 1994 Apr;23(4):669-73.

美喹他嗪物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 469.4±24.0 °C at 760 mmHg
• 熔点: 143-145ºC
• 分子式: C₂₀H₂₂N₂S
• 分子量: 322.467
• 闪点: 237.7±22.9 °C
• 精确质量: 322.150360
• PSA: 31.78000
• LogP: 5.38
• InChIKey: HOKDBMAJZXIPGC-UHFFFAOYSA-N
• SMILES: c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2
• 外观性状: 白色固体
• 蒸汽压: 0.0±1.2 mmHg at 25°C
• 折射率: 1.707
• 储存条件: Refrigerator
• 水溶解性: 水溶性：不溶；易溶于：甲醇；可溶于：乙醇

美喹他嗪毒性和生态

美喹他嗪安全信息

• 海关编码: 2934300000

美喹他嗪海关

• 海关编码: 2934300000
• 中文概述: 2934300000. 含一个吩噻嗪环系的化合物(吩噻嗪环系不论是否氢化,化合物未经进一步稠合的 ). 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途
• Summary: 2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

美喹他嗪靶点实验

查看更多实验

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression 来源：NCGC External Id：SNCA-p-activity-luciferase

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：Cytochrome P450 Family 1 Subfamily A Member 2 (CYP1A2) small molecule antagonists: lu... 来源：824 External Id：CYP273

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：qHTS for Inhibitors of TGF-b: Cytotox Counterscreen 来源：NCGC 靶标：N/A External Id：SMAD3201

实验名称：uHTS identification of cystic fibrosis induced NFkb Inhibitors in a fluoresence assay 来源：Burnham Center for Chemical Genomics 靶标：cystic fibrosis transmembrane conductance regulator [Homo sapiens] External Id：SBCCG-A764-CF-PAF-Primary-Assay

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ant... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_ANT_FLUO8_1536_1X%INH PRUN

实验名称：qHTS for Inhibitors of TGF-b 来源：NCGC 靶标：Smad3 [Homo sapiens] External Id：SMAD3101

实验名称：Primary qHTS for inhibitors of NSP2Pro chikungunya virus (CHIKV) 来源：NCGC External Id：APP-Toga-CHIKV-nsp2-p

实验名称：qHTS Assay for Identifying Compounds that block Entry of Ebola Virus, Screen 2 green ... 来源：NCGC 靶标：N/A External Id：Ebola screen2_EMI141217_green

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美喹他嗪英文别名

• EINECS 249-521-7
• Mequitazine
• Butix
• UNII:Y463242LY2
• Zesulan
• 10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine
• MFCD01706743