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  1. GPCR/G Protein
    Immunology/Inflammation
  2. Histamine Receptor

Histamine Receptor

Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

Histamine Receptor 相关产品 (123):

Cat. No.Product NameEffectPurity
  • HY-17043
    LoratadineAgonist 99.95%
    Loratadine(SCH-29851)是H1受体反向激动剂,IC50>32 μM。
  • HY-B1204
    HistamineActivator 99.96%
    Histamine是一种参与局部免疫反应的有机含氮化合物, 调节肠道生理功能, 且作为神经递质。
  • HY-N0054
    OstholeInhibitor 99.90%
    Osthole 是一种天然抗组胺药替代试剂。Osthole 可有效抑制组胺 H1 受体 (histamine H1receptor) 活性。
  • HY-14289
    CimetidineAntagonist >98.0%
    Cimetidine是H2受体拮抗剂。
  • HY-B0298A
    Clemastine fumarateAntagonist 99.82%
    Clemastine (fumarate) (HS-592 (fumarate)) 是组胺H1受体拮抗剂,IC50为 3 nM。
  • HY-111501
    H4R antagonist 1Antagonist
    H4R antagonist 1 是一种有效的高选择性组胺 H4 受体 (H4R) 拮抗剂,IC50 为 27 nM。H4R antagonist 1 对组胺受体的其他亚型 H1R,H2R 和 H3R 没有任何明显的结合亲和力。
  • HY-114025
    H4 Receptor antagonist 1Inhibitor 99.70%
    H4 Receptor antagonist 1 是一种有效的、有选择性的组胺H4受体 (H4R)的反向激动剂,其IC50 值为19 nM。
  • HY-15538
    EbrotidineAntagonist
    Ebrotidine(FI 3542)是竞争性H2受体拮抗剂,Ki为127.5nM,具有抗分泌活性,可用于胃保护。
  • HY-13508
    JNJ-7777120Antagonist 99.96%
    JNJ-7777120是一种选择性的组胺H4受体拮抗剂, Ki值为4 ±1 nM,比作用于其他组胺受体选择性高1000多倍。
  • HY-12199B
    Pitolisant hydrochlorideAntagonist 99.22%
    Pitolisant盐酸盐(BF2.649;Ciproxidine)是新型的人重组H3受体选择性反向激动剂,Ki为0.16 nM。
  • HY-14270
    LodoxamideInhibitor 98.00%
    Lodoxamide是作为肥大细胞稳定剂的抗过敏化合物, 用于治疗哮喘和过敏性结膜炎的。
  • HY-B0377
    FamotidineAntagonist 98.17%
    Famotidine (MK-208) 是组胺H2受体拮抗剂,可抑制胃液分泌。
  • HY-B0157A
    Ketotifen fumarateInhibitor 99.92%
    Ketotifen延胡索酸盐是第二代非竞争性H1抗组胺剂和肥大细胞稳定剂。
  • HY-B0801A
    Fexofenadine hydrochlorideInhibitor 99.61%
    Fexofenadine是第三代抗组胺药,用于治疗过敏症状,如花粉热,鼻塞和荨麻疹。
  • HY-15289
    Ciproxifan maleateAntagonist 99.56%
    Ciproxifan(FUB-359)马来酸盐是高活性的H3受体拮抗剂,IC50为9.2 nM,对其它亚型受体的亲和力较低。
  • HY-A0129
    Histamine phosphateAgonist 99.40%
    Histamine diphosphate是一个强的histamine受体的激活剂和血管扩张神经剂,能够激活一氧化氮合成酶。
  • HY-B0539
    DesloratadineAntagonist 99.75%
    Desloratadine(Sch34117)是人H1受体拮抗剂。
  • HY-B0164
    MizolastineAntagonist 99.33%
    Mizolastine是组胺H1受体拮抗剂,IC50为47 nM。
  • HY-B0349
    Meclizine dihydrochlorideAntagonist 99.97%
    Meclizine是H1组胺受体拮抗剂,可作用于晕动病。
  • HY-17042A
    Cetirizine dihydrochlorideInhibitor 99.17%
    Cetirizine二盐酸盐是第二代抗组胺剂,是hydroxyzine的主要代谢产物,是外消旋的选择性H1受体反向激动剂。
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