h4 receptor

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist with an IC50 of 19 nM.

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

ST-1006, a potent histamine H4 receptor agonist (pKi: 7.94), exhibits significant anti-inflammatory and anti-pruritic effects. It is also a potent inducer of basophil migration.

Alcaftadine (Lastacaft) is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.

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

Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4 receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).

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

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.

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).

VUF10460, a non-imidazole histamine H4 receptor agonist, [58C8-51-20-3] is structurally classified under the chlorobenzylpiperazine ethers with the IUPAC designation (2-[(2-chlorophenyl)methyl]-1-piperazinyl)(1H-indol-3-yl)methanone. It is typically utilized in pharmacological research and exhibits specificity for the H4 subtype, making it a valuable tool in immunological studies.

H4R antagonist 3 is a novel histamine-4 receptor (H4R) antagonist with an EC50 <10 mM.H4R antagonist 3 has potential inflammatory activity for the study of autoimmune, allergic and ocular diseases.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

BMH-7 (Histamine H4 receptor antagonist-2) is a p53 activator with antitumor activity through activation of the p53 pathway.

BMH-7 HCl is a p53 activator, showing anticancer activity through the activation of the p53 pathway.

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.

Adriforant hydrochloride is an antagonist of histamine H4 receptor.

H3R antagonist 5 (Compound 1b) is a selective inverse agonist of the histamine H3 receptor that can penetrate the blood-brain barrier, with an IC50 of 0.54 nM. It is applicable for research related to the central nervous system.

VUF 8430 dihydrobromide is a potent and selective histamine H4 receptor agonist with a Ki value of 31.6 nM and an EC50 of 50 nM, commonly used in immunology and inflammation research to investigate H4 receptor–mediated signaling, immune cell chemotaxis, cytokine release, and the role of histamine in allergic and inflammatory responses.

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.

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

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.