1. Signaling Pathways
  2. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  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 (129):

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-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-14289
    Cimetidine Antagonist >98.0%
    Cimetidine是H2受体拮抗剂。
  • 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-12532
    Astemizole Antagonist >98.0%
    Astemizole (R 43512) 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-121356
    Carebastine Antagonist
    Carebastine 是 Ebastine 的活性代谢产物。Carebastine 是一种组胺 H1 受体拮抗剂。Carebastine 抑制 VEGF 诱导的 HUVEC 和 HPAEC 增殖,迁移和血管生成。Carebastine 可抑制巨噬细胞移动抑制因子的表达。
  • 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-B1193
    Terfenadine Antagonist 98.26%
    Terfenadine ((±)-Terfenadine) 是一种有效的 hERG 开放通道抑制剂, IC50为 204 nM。Terfenadine 也是一种 H1 组胺受体 (histamine receptor) 拮抗剂,通过调节 Ca2+ 稳态在黑素瘤细胞中起到有效的细胞凋亡诱导作用。 Terfenadine 诱导 ROS 依赖性细胞凋亡,同时激活 Caspase-4,-2,-9,诱导 p73,Noxa
  • 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-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-B0801A
    Fexofenadine hydrochloride Inhibitor 99.61%
    Fexofenadine hydrochloride (MDL-16455 hydrochloride) 是一种 H1R 拮抗剂,可用于治疗季节性过敏性鼻炎和慢性特发性荨麻疹(针对年龄大于16岁的人)。
  • 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-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-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-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-B0781
    Promethazine hydrochloride Antagonist 99.82%
    Promethazine hydrochloride 是一代抗组胺药物,H1 受体强效拮抗剂和 mAChR 拮抗剂,对 5-HT2A、5-HT2C、D2和_alpha_1-adrenergic受体也有一定的亲和性。
  • HY-17042A
    Cetirizine dihydrochloride Inhibitor 99.17%
    Cetirizine dihydrochloride 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-B1090
    Cinnarizine Inhibitor 99.67%
    Cinnarizine是抗组胺剂和钙通道阻断剂, 促进脑血流, 用于治疗脑中风, 创伤后脑症状, 脑动脉硬化。
  • HY-B0539
    Desloratadine Antagonist 99.75%
    Desloratadine(Sch34117)是人H1受体拮抗剂。
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