(R)-(+)-Dimethindene maleate

Names

[ CAS No. ]:
136152-64-2

[ Name ]:
(R)-(+)-Dimethindene maleate

Biological Activity

[Description]:

(R)-(+)-Dimethindene maleate is an orally active H1-receptor blocker with antihistaminic properties in pigs[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H1 Receptor:7.7 (pA2)


[In Vitro]

(R)-(+)-Dimethindene maleate possesses membrane-stabilising effect[1].

[In Vivo]

(R)-(+)-Dimethindene maleate (10 mL/kg; i.g.; once) shows antihistaminic activity with an ED50 of 2.73 mg/kg in pigs[1]. Animal Model: Male guinea-pigs[1] Dosage: 10 mL/kg Administration: Oral gavage, once Result: The ED50-value for a protection from a fatal histamine shock was calculated as 2.73 mg/kg when administered orally 1 h before the injection of histamine. The calculated oral anti-anaphylactic ED50-value was found to be >31.6mg/kg. The oral LD50-values was found to be 988 mg/kg.

[References]

[1]. Leuschner J, et al. Evaluation of the dose-effect curves of dimethindene maleate enantiomers in various animal models. Agents and Actions, 1992, 36(2): C431-C433.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H28N2O4

[ Molecular Weight ]:
408.49


Related Compounds