VUF10460|VUF 10460|histamine H4 receptor agonist

Cas No.:	1028327-66-3
Synonyms:	VUF 10460,VUF-10460
SMILES:	CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3)N
Formula:	C₁₅H₁₉N₅
M.Wt:	269.34
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
Target:	pKi: 7.46 (H4)[1]
In Vivo:	HCl-induced rat gastric lesions is significantly enhanced by the H4 receptor agonists VUF10460. This effect is not modified by H4 receptor antagonist JNJ7777120[1].
In Vitro:	UF10460 binds to rat H3 and H4 receptor with pKi values of 5.75, and 7.46, respectively. VUF10460 displays approximately a 50-fold selectivity for the rat H4 receptor over the H3 receptor[1].
Animal Administration:	Rats: VUF10460 is dissolved in 100% DMSO. Gastric lesions are induced in 24 h fasted rats by a single intragastric administration of 0.6 N HCl (5mL/kg volume). Drugs under study are administered subcutaneously 30 min before HCl. Rats are randomly divided to receive single doses (10 and/or 30 mg/kg) of immethridine, methimepip, immepip, VUF8430, VUF10460 or the vehicle, in a 1 mL/kg volume[1].
References:	[1]. Coruzzi G, 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. 2011 Nov 1;669(1-3):121-7.

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