100130-32-3

VUF8430 is a histamine H₄ receptor agonist (K_i = 31.6 nM). It is selective for histamine H₄ over H₁ and H₃ receptors in radioligand binding assays (K_is = >1 and 1 μM, respectively) and is less active in isolated guinea pig atria, which endogenously expresses high levels of H₂ receptors (pD₂ = 3.8). VUF8430 inhibits forskolin-induced, cAMP-mediated increases in β-galactosidase activity (EC₅₀ = 50.1 nM). In vivo, VUF8430 (30 mg/kg) enhances HCl-induced formation of gastric lesions in rats. It also reduces mechanical and thermal allodynia in a mouse model of peripheral neuropathy induced by spared nerve injury (SNI).

VUF 8430 Dihydrobromide is an H4 receptor agonist.

H₄ receptor

Desiccate at RT

[1] HERMAN D. LIM. Discovery of S-(2-Guanidylethyl)-isothiourea (VUF 8430) as a Potent Nonimidazole Histamine H4 Receptor Agonist[J]. Journal of Medicinal Chemistry, 2006, 49 23: 6650-6651. DOI: 10.1021/jm060880d
[2] GABRIELLA CORUZZI . Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach[J]. European journal of pharmacology, 2011, 669 1: Pages 121-127. DOI: 10.1016/j.ejphar.2011.07.038
[3] MARIA DOMENICA SANNA. Histamine H4 receptor agonist-induced relief from painful peripheral neuropathy is mediated by inhibition of spinal neuroinflammation and oxidative stress[J]. British Journal of Pharmacology, 2016, 174 1: 28-40. DOI: 10.1111/bph.13644