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VUF 10460

Names

[ CAS No. ]:
1028327-66-3

[ Name ]:
VUF 10460

[Synonym ]:
2-Pyrimidinamine, 4-(4-methyl-1-piperazinyl)-6-phenyl-
4-(4-Methyl-1-piperazinyl)-6-phenyl-2-pyrimidinamine
VUF10460

Biological Activity

[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.


[Related Small Molecules]

Loratadine | Histamine | Pitolisant hydrochloride | Cimetidine | Osthole | Clemastine fumarate | Ebrotidine | JNJ-7777120 | Famotidine | Cetirizine Dihydrochloride | Desloratadine | Ketotifen fumarate | Lodoxamide | Meclizine dihydrochloride | Chlorpheniramine maleate

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
523.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H19N5

[ Molecular Weight ]:
269.345

[ Flash Point ]:
270.6±32.9 °C

[ Exact Mass ]:
269.164032

[ LogP ]:
1.27

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.621

[ Storage condition ]:
2-8℃

Related Compounds