2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐

• 常用名: 2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐
• 英文名: Triprolidine hydrochloride
• CAS号: 550-70-9
• 分子量: 314.85200
• 密度: 1.061g/cm3
• 沸点: 435.4ºC at 760mmHg
• 分子式: C₁₉H₂₃ClN₂
• 熔点: 59-61ºC
• 闪点: 217.1ºC

用途

Triprolidine 是一种有口服活性的,第一代组胺 H1 受体 (histamine H1-receptor) 拮抗剂,可用于过敏性鼻炎的研究。在大鼠中,Triprolidine 能阻滞脊髓运动和感觉。

名称

• 中文名: 2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐
• 英文名: triprolidine hydrochloride (anh.)
• 中文别名: 盐酸曲普立定

生物活性

• 描述: Triprolidine 是一种有口服活性的,第一代组胺 H1 受体 (histamine H1-receptor) 拮抗剂,可用于过敏性鼻炎的研究。在大鼠中,Triprolidine 能阻滞脊髓运动和感觉。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 靶点实验:

  H1 Receptor

• 体内研究: 曲普利啶(292.81-1467.20μg/kg；鞘内注射)对大鼠脊髓运动和感觉阻滞产生剂量依赖性效应[3]。动物模型：雄性Sprague-Dawley大鼠(300-350 g)[3]剂量：292.81μg/kg,488.02μg/kg,733.60μg/kg,1098.83μg/kg,1467.20μg/kg给药：鞘内注射结果：诱发剂量依赖性脊髓阻滞。
• 参考文献:

  [1]. K J Simons, et al. An investigation of the H1-receptor antagonist triprolidine: pharmacokinetics and antihistaminic effects. J Allergy Clin Immunol. 1986 Feb;77(2):326-30.

  [2]. D L Deal, et al. Disposition and metabolism of triprolidine in mice. Drug Metab Dispos. Nov-Dec 1992;20(6):920-7.

  [3]. Jann-Inn Tzeng, et al. Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats. J Pharm Pharmacol. 2018 Dec;70(12):1654-1661.

物理化学性质

• 密度: 1.061g/cm3
• 沸点: 435.4ºC at 760mmHg
• 熔点: 59-61ºC
• 分子式: C₁₉H₂₃ClN₂
• 分子量: 314.85200
• 闪点: 217.1ºC
• 精确质量: 314.15500
• PSA: 16.13000
• LogP: 4.65740
• InChIKey: WYUYEJNGHIOFOC-UHFFFAOYSA-N
• SMILES: Cc1ccc(C(=CCN2CCCC2)c2ccccn2)cc1.Cl
• 储存条件: 2-8°C

毒性和生态

安全信息

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 22-36/37/38
• 安全声明 (欧洲): 26-36
• 危险品运输编码: UN 3249
• WGK德国: 3
• RTECS号: UT7658000
• 包装等级: III
• 危险类别: 6.1(b)
• 海关编码: 2933990090

海关

• 海关编码: 2933990090
• 中文概述: 2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
• Summary: 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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：Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 来源：ChEMBL 靶标：N/A External Id：CHEMBL1266185

实验名称：ERK5 transcriptional activity HTS 来源：24565 靶标：N/A External Id：ERK5 transcriptional activity-HTS

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

共172条，当前第1页，共18页

1

2

3

4

5

英文别名

• EINECS 208-985-0
• MFCD00039044
• Triprolidine Hydrochloride
• Triprolidine HCl