1. Signaling Pathways
  2. GPCR/G Protein
  3. 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 (125):

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-B1204
    Histamine Activator 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-14289
    Cimetidine Antagonist >98.0%
  • 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-B0298A
    Clemastine fumarate Antagonist 99.82%
    Clemastine (fumarate) (HS-592 (fumarate)) 是组胺H1受体拮抗剂,IC50为 3 nM。
  • HY-111501
    H4R antagonist 1 Antagonist
    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-B1101A
    Pimethixene maleate Antagonist
    Pimethixene maleate 是抗组胺和抗血清素剂,用作抗偏头疼剂。Pimethixene maleate 为高效的多靶点拮抗剂,对 5-HT1A,5-HT2A,5-HT2B,5-HT2C,组胺 H1,多巴胺 D2 和 D4.4 以及毒蕈碱 M1 和 M2pKi 值分别为 7.63,10.22,10.44,8.42,10.14,8.19,7.54,8.61 和 9.38。
  • HY-12532
    Astemizole Antagonist
    Astemizole 是一个长效的二代抗组胺药物,是常用的抗过敏药物,是组胺H1 受体 (histamine H1-receptor) 的拮抗剂,IC50 值为 4 nM。Astemizole 同时还具有hERG K+通道的阻断活性,IC50 值为0.9 nM。Astemizole 还具有抗胆碱能和止痒作用。
  • 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-13508
    JNJ-7777120 Antagonist 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 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-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-B0377
    Famotidine Antagonist 98.17%
    Famotidine (MK-208) 是组胺H2受体拮抗剂,可抑制胃液分泌。
  • HY-B0801A
    Fexofenadine hydrochloride Inhibitor 99.61%
  • HY-B0157A
    Ketotifen fumarate Inhibitor 99.92%
  • HY-17042A
    Cetirizine dihydrochloride Inhibitor 99.17%
  • 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-14537
    Latrepirdine dihydrochloride Antagonist 99.75%
    Latrepirdine dihydrochloride 是一种神经活性化合物,对组胺受体 (histaminergic receptor),α-肾上腺素能受体 (α-adrenergic receptor) 和 5-羟色胺受体 (serotonergic receptor) 具有拮抗活性。Latrepirdine 刺激淀粉样前体蛋白 (APP) 分解代谢和 β-淀粉样蛋白 (amyloid-β, ) 分泌。
  • HY-A0129
    Histamine phosphate Agonist 99.79%
    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-B0164
    Mizolastine Antagonist 99.33%
    Mizolastine是组胺H1受体拮抗剂,IC50为47 nM。
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