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 (123):

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-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-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-14289
    Cimetidine Antagonist >98.0%
  • 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-111501
    H4R antagonist 1 Antagonist
    H4R antagonist 1 是一种有效的高选择性组胺 H4 受体 (H4R) 拮抗剂,IC50 为 27 nM。H4R antagonist 1 对组胺受体的其他亚型 H1R,H2R 和 H3R 没有任何明显的结合亲和力。
  • HY-114025
    H4 Receptor antagonist 1 Inhibitor 99.70%
    H4 Receptor antagonist 1 是一种有效的、有选择性的组胺H4受体 (H4R) 的反向激动剂,其IC50 值为19 nM。
  • HY-12190
    JNJ-5207852 Antagonist >98.0%
    JNJ-5207852 是组胺 H3 受体有选择性的有效拮抗剂,其对大鼠和人类 H3 受体的 pKi 值分别为 8.9,9.24。
  • 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-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-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-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-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-B0157A
    Ketotifen fumarate Inhibitor 99.92%
  • HY-B0801A
    Fexofenadine hydrochloride Inhibitor 99.61%
  • 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-A0129
    Histamine phosphate Agonist 99.40%
    Histamine diphosphate是一个强的histamine受体的激活剂和血管扩张神经剂,能够激活一氧化氮合成酶。
  • HY-B0539
    Desloratadine Antagonist 99.75%
  • HY-B0164
    Mizolastine Antagonist 99.33%
    Mizolastine是组胺H1受体拮抗剂,IC50为47 nM。
  • HY-B0349
    Meclizine dihydrochloride Antagonist 99.97%
Isoform Specific Products

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