1. GPCR/G Protein
  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 (98):

Cat. No. Product Name Effect Purity
  • 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-A0077
    Perphenazine Inhibitor 99.93%
    Perphenazine 是一种典型的抗精神病药物, 抑制5-HT2A 受体(5-HT2A), Alpha-1A肾上腺素受体(α1A), 多巴胺受体D2/D3, D2L, 和组胺 H1 受体 (H1), Ki值分别为5.6, 10, 0.765/0.13, 3.4, 和 8 nM.
  • HY-N0054
    Osthole Inhibitor 99.81%
    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 99.80%
    Clemastine延胡索酸盐是组胺H1受体拮抗剂,IC50为3 nM。
  • HY-30234A
    Clemizole hydrochloride Antagonist 99.70%
    Clemizole hydrochloride 是一种 H1 组胺受体 (H1 histamine receptor) 拮抗剂,抑制 HCV 复制。
  • HY-16289
    Lodoxamide tromethamine Inhibitor >98.0%
    Lodoxamide tromethamine是治疗肥大细胞介导的过敏性疾病的药物。
  • HY-B1510
    Acrivastine Inhibitor 98.00%
    Acrivastine (BW825C) 是用于治疗过敏性鼻炎的短效histamine 1受体拮抗剂。
  • HY-101420
    VUF10460 Agonist 98.37%
    VUF10460是非咪唑组胺H4受体激动剂; 与大鼠H4受体结合的pKi值为7.46。
  • HY-B0781
    Promethazine hydrochloride Antagonist 99.82%
  • HY-A0015
    Bepotastine Beslilate Antagonist 99.36%
    Bepotastine Beslilate (Bepreve)是组胺H1受体拮抗剂。
  • HY-B1204
    Histamine Activator 98.08%
    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-B0377
    Famotidine Antagonist 99.26%
  • HY-B0462
    Azelastine hydrochloride Antagonist 99.97%
  • HY-B0970
    Diphenylpyraline hydrochloride Inhibitor 98.41%
    Diphenylpyraline盐酸盐是第一代抗组胺剂, 具有抗胆碱能作用, 充当多巴胺再摄取抑制剂, 可用于治疗帕金森症。
  • HY-15538
    Ebrotidine Antagonist 98.44%
    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-B0539
    Desloratadine Antagonist 99.91%
  • HY-17039
    Alcaftadine Antagonist
  • HY-B0349
    Meclizine dihydrochloride Antagonist 99.81%
  • HY-14447
    Bilastine Antagonist 99.95%
  • HY-17042A
    Cetirizine dihydrochloride Inhibitor >98.0%