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

European Journal of Pharmacology
S MorissetJ C Schwartz

Abstract

Following tacrine administration i.p. to mice, the histamine N-methyltransferase activity of brain homogenates was more potently inhibited than the acetylcholinesterase activity (ID50 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 H3 receptor antagonist was abolished by tacrine with an ID50 as low as 1.2 +/- 0.4 mg/kg. The participation of histamine in the actions of tacrine and the relevance of histamine H3 receptor antagonists in Alzheimer's disease are suggested.

References

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Citations

Oct 20, 2001·Behavioural Brain Research·L BacciottiniP Blandina
Nov 13, 2001·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·J C SchwartzJ M Arrang
Jun 1, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·G MeierH Stark
May 4, 2002·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Sven GrassmannWalter Schunack
Mar 11, 2000·The European Journal of Neuroscience·M NishiboriK Saeki
Jan 12, 2010·Behavioural Brain Research·E DereJ P Huston
Sep 20, 2005·Journal of Molecular Biology·John R HortonXiaodong Cheng
May 31, 2015·Neuropharmacology·Armin ZlomuzicaEkrem Dere
Oct 24, 2013·European Journal of Medicinal Chemistry·Manjinder SinghDhandeep Singh
Jun 30, 2007·Journal of Pharmacological Sciences·Yasuko YamamotoChiaki Kamei
Dec 15, 2010·Thérapie·Mouhammad MotawajJean-Michel Arrang
Oct 22, 2016·European Journal of Medicinal Chemistry·Hena Khanam Shamsuzzaman
Jun 12, 2002·Bioorganic & Medicinal Chemistry·Galina MeierHolger Stark
Apr 24, 2015·The Analyst·Srimal SamaranayakeParastoo Hashemi
Nov 15, 2008·Archiv der Pharmazie·Iwona Maslowska-LipowiczKrzysztof Walczynski
Nov 9, 2010·The Journal of Pharmacology and Experimental Therapeutics·M MotawajJ-M Arrang

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