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 (173):

Cat. No. Product Name Effect Purity
  • 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 99.95%
    Clemastine (fumarate) (HS-592 (fumarate)) 是组胺H1受体拮抗剂,IC50为 3 nM。
  • HY-17043
    Loratadine Agonist 99.95%
    Loratadine(SCH-29851) 是 histamine H1 受体反向激动剂,IC50>32 μM。Loratadine 具有抗登革热病毒 (DENV) 的活性。
  • HY-B1193
    Terfenadine Antagonist 99.93%
    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
  • 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-I0021
    Bepotastine Antagonist 98.12%
    Bepotastine 是一种具有口服活性的第二代组胺 H1 受体拮抗剂。Bepotastine 可用于过敏性鼻炎和荨麻疹/瘙痒症的研究。
  • HY-123812
    PF-03654764 Antagonist >99.0%
    PF-03654764 是一种具有口服活性的,选择性组胺 H3 受体拮抗剂,对人 H3 和大鼠 H3Ki 值分别为 1.2 nM 和 7.9 nM。PF-03654764 和 Fexofenadine (HY-B0801A) 组合具有用于过敏性鼻炎研究的潜力。
  • HY-101198
    Clobenpropit dihydrobromide Modulator
    Clobenpropit dihydrobromide 是一种有效的组胺 H3R 拮抗剂/反向激动剂,对组胺 H3LR 的 pEC 50 为 8.07。Clobenpropit dihydrobromide 对组胺 H4 受体起部分激动剂的作用,Ki 为 13 nM。Clobenpropit dihydrobromide 还与 5-HT3 受体 (Ki 为 7.4 nM) 和 α2A/α2C 肾上腺素受体 (Ki 为 17.4/7.8 nM) 结合。Clobenpropit dihydrobromide 促进凋亡 (apoptosis)。
  • HY-12199B
    Pitolisant hydrochloride Antagonist 99.67%
    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-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。Osthole 还可抑制细胞培养物中 HBV 的分泌。
  • HY-14289
    Cimetidine Antagonist >98.0%
    Cimetidine是H2受体拮抗剂。
  • HY-17042A
    Cetirizine dihydrochloride Antagonist 99.17%
    Cetirizine dihydrochloride 是羟嗪的羧化代谢物,是第二代抗组胺药。Cetirizine dihydrochloride 是一种特异的、口服有效的、H1 受体 的长效拮抗剂。Cetirizine dihydrochloride 标记抗过敏特性,抑制过敏反应期间嗜酸性粒细胞趋化。
  • 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-A0077
    Perphenazine Inhibitor 99.90%
    Perphenazine 是一个经典的抗精神病药物,能够抑制 5-HT2A 受体,α1A 肾上腺素能受体,多巴胺D2/D3、D2L 受体, 以及 组胺H1 受体,对应的 Ki 值分别为5.6,10,0.765/0.13,3.4 和8 nM。
  • HY-13511A
    Rupatadine Fumarate Antagonist 99.93%
    Rupatadine Fumarate (UR-12592 Fumarate) 富马酸盐是 PAF/H1 受体双抑制剂,Ki 值分别为0.55 μM 和 0.1 μM。
  • HY-14270
    Lodoxamide Inhibitor 99.71%
    Lodoxamide (U-42585E free acid) 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-12532
    Astemizole Antagonist 99.68%
    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-B0188A
    Mianserin hydrochloride Inhibitor 99.85%
    Mianserin hydrochloride (Org GB 94) 是 H1 受体反向激动剂,有抗抑郁活性。
  • HY-B0157A
    Ketotifen fumarate Inhibitor 99.83%
    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-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。
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