human h4 receptor

JNJ-39758979是一种选择性的、高亲和力的、可口服的组胺 H4 受体拮抗剂，具有抗炎和止痒作用，对人、小鼠和猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。它对组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。

H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.

Toreforant is an effective and selective histamine H4 receptor antagonist (Ki at the human receptor: 8.4 nM).

PF-03654764对人类H3受体具有高亲和力，并对大鼠H3受体具有较低亲和力，同时对其他人类组胺受体亚型（H1，H2和H4）具有超过1000倍的选择性。在使用报告基因测定法（β-内酰胺酶）并在稳定表达全长人类或大鼠H3受体的HEK293细胞中测量cAMP的功能性实验中，PF-03654764展示了强大的拮抗剂特性。

JNJ 10191584 maleate (VUF6002 maleate) 是一种具有口服活性的选择性 H4 受体拮抗剂 (Ki = 26 nM)。 JNJ 10191584 maleate 抑制嗜酸性粒细胞和肥大细胞的趋化性(IC50 = 530 nM 和 138 nM)。

A-940894 is a histamine H4 receptor antagonist with anti-inflammatory properties. A-940894 potently binds to both human and rat histamine H4 receptors and exhibits considerably lower affinity for the human histamine H1, H2, or H3 receptors. A-940894 has g

VUF-10497 is a histamine H4 receptor inverse agonist (pKi = 7.57). VUF-10497 was found to possess anti-inflammatory properties in vivo in the rat. VUF-10497 also possesses a considerable affinity for the human histamine H1 receptor.

JNJ-10191584, a potent and selective antagonist at the histamine H4 receptor, has antiinflammatory and analgesic effects in animal studies of acute inflammation.

UR-PI376 is a histamine H4 receptor agonist (hH4R agonist) (pEC50 = 7.47, alpha = 0.93), with low activity for hH1R and hH2R and significant selectivity for hH3R (pKB = 6.00, alpha =- 0.28), as in stable-use a membrane preparation of hH(x)R-expressing Sf9

UR-RG98 is a potent and selective agonist of human histamine H4 receptor (hH4R).

Izuforant (JW1601) (Compound 24) 具有有效的抗炎和止痒活性。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力，IC50值为 9.1 μM。它也是组胺 H4 受体 (H4R) 的口服活性拮抗剂，对人 H4R 的IC50值为 36 nM。

INCB38579 是一种选择性的、口服具有活力的、能够透过血脑屏障的组胺 H4受体 (HH4R) 拮抗剂，能够作用于 hH4R (IC50: 4.8 nM)、mH4R (IC50: 42 nM)、rH4R (IC50: 32 nM)。INCB38579 具有抗炎和抗瘙痒作用。

Adriforant tartrate hydrate, also known as ZPL-3893787 tartrate hydrate, PF-3893787 tartrate hydrate and ZPL-389 tartrate hydrate, is a novel histamine H4 receptor antagonist. Adriforant tartrate hydrate shows an excellent in vitro profile that warrants their further investigation in relevant models of human disease. Histamine H4 receptor (H4R) has become a promising target for immuno-inflammatory diseases, such as allergic rhinitis, asthma or dermal allergies.

A-943931 是一种有效的选择性组胺 H4 受体拮抗剂，对人和大鼠 H4R 的 Ki 值分别为 4.6、3.8 nM。A-943931 具有抗炎和抗伤害作用。

Clobenpropit dihydrobromide 是一种组胺H3R 拮抗剂 反向激动剂。它与 5-HT3 受体和 α2A α2C 肾上腺素受体结合，对组胺H4受体起部分激动剂的作用，还能促进凋亡。