基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 新闻专题 供应信息 相关产品
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富马酸卢帕他定

基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 新闻专题 供应信息 相关产品
富马酸卢帕他定
富马酸卢帕他定 性质
  • 熔点 196-198°C
  • 储存条件 Refrigerator
富马酸卢帕他定 用途与合成方法
  • 生物活性Rupatadine Fumarate是一种PAFR和组胺(H1)受体抑制剂,Ki分别为550 nM和102 nM。
  • 体外研究Rupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29 ?0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4(LTD4). It also competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2= 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation. In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α.
  • 体内研究Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 μg/kg i.v.). Moreover, it potently inhibits PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.). Rupatadine's duration of action is long, as assessed by the histamine- and PAF-induced increase in vascular permeability test in dogs (42 and 34% inhibition at 26 h after 1 mg/kg p.o.). Rupatadine at a dose of 100 mg/kg p.o. neither modifies spontaneous motor activity nor prolongs barbiturate-sleeping time in mice, which indicates a lack of sedative effects.
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  • 公司名称:上海波以尔化工有限公司
  • 联系电话:
  • 产品介绍: 英文名称:Rupatadine Fumarate
    CAS:182349-12-8
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  • 公司名称:百灵威科技有限公司
  • 联系电话:400-666-7788 +86-10-82848833
  • 产品介绍: 中文名称:卢帕他定
    英文名称:Rupatadine FuMarate
    CAS:182349-12-8
    包装信息:1g,250Mg,5g 备注:化学试剂、精细化学品、医药中间体、材料中间体
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  • 公司名称:上海佰世凯化学科技有限公司
  • 联系电话:+86(0)21-20908456
  • 产品介绍: 英文名称:Rupatadine fuMarate
    CAS:182349-12-8
    备注:C14132
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  • 公司名称:凯方医药科技(上海)有限公司
  • 联系电话:021-67220633 & 021-37212706
  • 产品介绍: 英文名称:8-Chloro-6,11-dihydro-11-[1-[(5-Methyl-3-pyridyl)Methyl]-4-piperidylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine fuMarate
    CAS:182349-12-8
    纯度:99% 包装信息:5KG;1KG
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  • 公司名称:南京康满林化工实业有限公司
  • 联系电话:025-83697070
  • 产品介绍: 中文名称:富马酸卢帕他定
    英文名称:8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine fumarate
    CAS:182349-12-8
    纯度:98.00% 包装信息:10g;500g;1kg;10kg 备注:950元/25g,98%现货
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