human 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

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 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.

JNJ 10191584 maleate (VUF6002 maleate) is an orally active and selective antagonist of H4 receptor (Ki = 26 nM). JNJ 10191584 maleate inhibits chemotaxis of eosinophils and mast cells (IC50 = 530 nM and 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) exhibits potent anti-inflammatory and anti-pruritic activities, with a binding affinity for human serotonin 3 receptor (h5-HT3R) and an IC50 value of 9.1 μM. It is also an orally active antagonist of histamine H4 receptor (H4R), showing an IC50 value of 36 nM against human H4R [1] [2].

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.

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 is a selective histamine H4 receptor antagonist with human and rat Ki values of 4.6 and 3.8 nM respectively. It inhibits the scratching response in mice and exhibits anti-pruritic activity.

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