rat h4 receptor

JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2

PF-03654764 exhibits high affinity for the human H3 receptor, but displays significantly lower affinity for the rat H3 receptor, with over 1000-fold selectivity against other human histamine receptor subtypes (H1, H2, and H4). In functional assays measuring cAMP using reporter gene assays (β-lactamase) conducted in HEK293 cells stably expressing the full-length human or rat H3 receptor, PF-03654764 demonstrated potent antagonist properties.

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-10214 is an H4 receptor-ligand. VUF-10214 has significant anti-inflammatory properties in the carrageenan-induced paw edema model in vivo studies in the rat reveal.

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.

INCB38579 is a selective, orally active, histamine H4 receptor (HH4R) antagonist that crosses the blood-brain barrier and acts on hH4R (IC50: 4.8 nM), mH4R (IC50: 42 nM), and rH4R (IC50: 32 nM). INCB38579 has anti-inflammatory and antipruritic effects.

A-943931, a selective and potent antagonist of the histamine H4 receptor (H4R), demonstrates affinity with pKi values of 4.6 and 3.8 nM for human and rat H4Rs, respectively. This compound exhibits anti-inflammatory and antinociceptive properties.

Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)