vuf10460

Description: VUF10460 is a non-imidazole agonist of the histamine H4 receptor which binds to rat H4 receptor with a pKi of 7.46. Radioligand binding studies showed that VUF10460 displayed approximately a 50-fold selectivity for the rat H4 receptor over the H3 receptor, VUF10460, possibly due to the lack of imidazole heterocycle. In conscious rats, immethridine and methimepip significantly reduced (66% and 48% inhibition, respectively) the gastric lesions induced by HCl; HCl-induced lesions were also significantly enhanced by the H4 receptor agonists VUF10460 and VUF8430, suggesting the activation of histamine H4 receptors by the selective agonists VUF10460 and VUF8430 aggravated the ulcerogenic effects of 0.6 N HCl.

References: Pharmacology. 2012; 89(5-6):287-94; Eur J Pharmacol. 2011 Nov 1; 669(1-3):121-7.