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 (122):

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 99.25%
    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-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-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-14289
    Cimetidine Antagonist >98.0%
    Cimetidine是H2受体拮抗剂。
  • HY-112067A
    Chlorcyclizine hydrochloride Antagonist 99.90%
    Chlorcyclizine hydrochloride 是一种组胺 H1 拮抗剂。
  • HY-16344
    Nedocromil sodium Inhibitor
    Nedocromil sodium 抑制多种介质的作用或形成,包括组胺,白三烯 C4 (LTC4) 和前列腺素 D2 (PGD2)。
  • HY-16756
    Toreforant Antagonist
    Toreforant 是组胺 H4 (H4R) 受体一个有效的、选择性拮抗剂,人类中的 Ki 值为 8.4 nM。
  • 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-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-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-B0377
    Famotidine Antagonist 98.17%
    Famotidine是组胺H2受体拮抗剂,可抑制胃液分泌。
  • 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。
  • HY-B0781
    Promethazine hydrochloride Antagonist 99.82%
    Promethazine盐酸盐(NSC-231688)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-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-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-B0801A
    Fexofenadine hydrochloride Inhibitor 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-B0303A
    Diphenhydramine hydrochloride Antagonist 99.75%
    Diphenhydramine(Benadryl)盐酸盐是组胺H1拮抗剂。
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