ROS 234 dioxalate

Names

[ CAS No. ]:
1781941-93-2

[ Name ]:
ROS 234 dioxalate

Biological Activity

[Description]:

ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H2 Receptor:8.90 (pKi, Rat cerebral cortex H3-receptor)

[In Vivo]

ROS 234, centrally injected, significantly shortens pentobarbital narcosis[1].

[References]

[1]. Ballabeni V, et al. CNS access of selected H3-antagonists: ex vivo binding study in rats. Inflamm Res. 2002 Apr;51 Suppl 1:S55-6.

[2]. Mor M, et al. Synthesis, biological activity, QSAR and QSPR study of 2-aminobenzimidazole derivatives as potent H3-antagonists. Bioorg Med Chem. 2004 Feb 15;12(4):663-74.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₉N₅O₈

[ Molecular Weight ]:
421.36

Related Compounds

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