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(R)-Dimethindene Maleate is a subtype-selective mAChR M2 antagonist and histamine H1 receptor antagonist. | [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.
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H1 Receptor: 7.7 (pA2) |
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