1028327-66-3

1028327-66-3 structure

Name: VUF 10460
Chemical Name: 4-(4-Methyl-1-piperazinyl)-6-phenyl-2-pyrimidinamine
CAS Number: 1028327-66-3
Molecular Formula: C₁₅H₁₉N₅
Molecular Weight: 269.345
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-06-15 14:37:41
Modify Date: 2024-01-04 09:56:30
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.

Name	4-(4-Methyl-1-piperazinyl)-6-phenyl-2-pyrimidinamine
Synonyms	2-Pyrimidinamine, 4-(4-methyl-1-piperazinyl)-6-phenyl- 4-(4-Methyl-1-piperazinyl)-6-phenyl-2-pyrimidinamine VUF10460

Description	VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology
Target	pKi: 7.46 (H4)[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].
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].
Animal Admin	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.