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 (105):

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-14289
    Cimetidine Antagonist >98.0%
  • 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-12537
    Peptide 401 Antagonist 98.29%
    Peptide 401 是一种有效的来源于蜂毒中的肥大细胞脱颗粒肽,抑制血管通透性。
  • HY-19705B
    PF-3893787 hydrochloride Antagonist >98.0%
    PF-3893787 hydrochloride 是一种新型组胺 H4 受体亲和型拮抗剂 (Ki=2.4 nM),也是一种H4 受体功能性拮抗剂 (Ki=1.56 nM)。
  • HY-104003
    S 38093 Antagonist 99.02%
    S 38093 是一种大脑渗透的 H3 receptor 拮抗剂,对大鼠,小鼠和人的 H3 受体具有不同的亲和力,Ki 值分别为 8.8,1.44 和 1.2 µM。
  • 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 >98.0%
    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-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-17043
    Loratadine Agonist 99.81%
    Loratadine(SCH-29851)是H1受体反向激动剂,IC50>32 μM。
  • HY-B0539
    Desloratadine Antagonist 99.91%
  • HY-B0462
    Azelastine hydrochloride Antagonist 99.95%
  • 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-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-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-B0781
    Promethazine hydrochloride Antagonist 99.82%
  • HY-17039
    Alcaftadine Antagonist
  • HY-A0015
    Bepotastine Beslilate Antagonist 99.36%
    Bepotastine Beslilate (Bepreve)是组胺H1受体拮抗剂。