Description
VUF8430 is a histamine H
4 receptor agonist (K
i = 31.6 nM). It is selective for histamine H
4 over H
1 and H
3 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 H
2 receptors (pD
2 = 3.8). VUF8430 inhibits forskolin-induced, cAMP-mediated increases in β-galactosidase activity (EC
50 = 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).
