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 (121):

Cat. No. Product Name Effect Purity
  • HY-17043
    Loratadine Agonist 99.95%
    Loratadine(SCH-29851)是H1受体反向激动剂,IC50>32 μM。
  • HY-12199B
    Pitolisant hydrochloride Antagonist 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-B1204
    Histamine Activator 99.25%
    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-15538
    Ebrotidine Antagonist
    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-14289
    Cimetidine Antagonist >98.0%
    Cimetidine是H2受体拮抗剂。
  • HY-B1281
    Mepyramine maleate Antagonist >99.0%
    Mepyramine maleate 是第一代抗组胺剂,为 histamine H1 受体拮抗剂,对 H1,H2 和 H3 受体的 Kd 值分别为 0.8 nM,5200 nM 和 >3000 nM,对 H1 受体的 pKd 值为 9.4。
  • HY-112067A
    Chlorcyclizine hydrochloride Antagonist 99.90%
    Chlorcyclizine hydrochloride 是一种组胺 H1 拮抗剂。
  • HY-112219A
    H3R-IN-1 Hydrochloride Inhibitor
    H3R-IN-1 Hydrochloride 是一种有效的组胺受体 3 (H3R) 反向激动剂,详细信息请参考专利文献 WO2013107336A1 中的化合物 2。
  • HY-13508
    JNJ-7777120 Antagonist 98.13%
    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-N0054
    Osthole Inhibitor 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 H1 receptor) 活性。
  • HY-30234A
    Clemizole hydrochloride Antagonist 99.32%
    Clemizole hydrochloride 是一种 H1 组胺受体 (H1 histamine receptor) 拮抗剂,抑制 HCV 复制。
  • HY-B0298A
    Clemastine fumarate Antagonist 99.82%
    Clemastine延胡索酸盐是组胺H1受体拮抗剂,IC50为3 nM。
  • HY-B0377
    Famotidine Antagonist 98.17%
    Famotidine是组胺H2受体拮抗剂,可抑制胃液分泌。
  • HY-15289
    Ciproxifan maleate Antagonist 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-17042A
    Cetirizine dihydrochloride Inhibitor 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。
  • HY-B0462
    Azelastine hydrochloride Antagonist 99.95%
    Azelastine盐酸盐是第二代H1受体拮抗剂。
  • HY-B0157A
    Ketotifen fumarate Inhibitor 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-12195
    ABT-239 Antagonist 98.94%
    ABT-239 是一种新颖的,高效的,非咪唑类的 H3R 拮抗剂,也是 TRPV1 的拮抗剂。
  • HY-14270
    Lodoxamide Inhibitor 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-B0539
    Desloratadine Antagonist 99.75%
    Desloratadine(Sch34117)是人H1受体拮抗剂。
Isoform Specific Products

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