histamine h4 receptor antagonist 1

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor.

H4 Receptor antagonist 1 是选择性组胺 H4受体反向激动剂，其IC50值为19 nM。

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.

A-943931 is a histamine H4receptor antagonist (Ki= 3.8 nM).1In vivo, A-943931 inhibits scratching induced by clobenpropit in mice (ED50= 26 μmoles/kg, i.p.). 1.Milicic, I., Witte, D.G., Miller, T.L., et al.Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activityFASEB J.23(S1)760.768-760.768(2009)

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。

H4R antagonist 2 是Furo[3,2-d]嘧啶衍生的有效H4R拮抗剂，主要用于类风湿性关节炎的研究。