VUF8430 (hydrobromide)

VUF8430 is a histamine H₄ receptor agonist (K_i = 31.6 nM).¹ 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.² It also reduces mechanical and thermal allodynia in a mouse model of peripheral neuropathy induced by spared nerve injury (SNI).³

WARNING This product is not for human or veterinary use.

1. Lim, H.D., Smits, R.A., Bakker, R.A., et al. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J. Med. Chem. 49(23), 6650-6651 (2006).

2. Coruzzi, G., Adami, M., Pozzoli, C., et al. Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur J. Pharmacol. 669(1-3), 121-127 (2011).

3. Sanna, M.D., Lucarini, L., Durante, M., et al. Histamine H4 receptor agonist-induced relief from painful peripheral neuropathy is mediated by inhibition of spinal neuroinflammation and oxidative stress. Br. J. Pharmacol. 174(1), 28-40 (2017).