Inhibition of histamine versus acetylcholine metabolism as a mechanism of tacrine activity

Abstract : Following tacrine administration i.p. to mice, the histamine N -methyltransferase activity of brain homogenates was more potently inhibited than the acetylcholinesterase activity (ID 50 of 5.3 mg/kg vs. 13.6 mg/kg). The formation of the metabolite, tele-methylhistamine, in brain of mice treated with an histamine H 3 receptor antagonist was abolished by tacrine with an ID 50 as low as 1.2 ± 0.4 mg/kg. The participation of histamine in the actions of tacrine and the relevance of histamine H 3 receptor antagonists in Alzheimer's disease are suggested.
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Séverine Morisset, Elisabeth Traiffort, Jean-Charles Schwartz. Inhibition of histamine versus acetylcholine metabolism as a mechanism of tacrine activity. European Journal of Pharmacology, Elsevier, 1996, 315 (1), pp.R1-R2. ⟨10.1016/s0014-2999(96)00738-8⟩. ⟨hal-02081407⟩

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