Reference : Comparative study of pirlindole, a selective RIMA, and its two enantiomers using biochem...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/35323
Comparative study of pirlindole, a selective RIMA, and its two enantiomers using biochemical and behavioural techniques.
English
Bruhwyler, J. [> > > >]
Liégeois, Jean-François mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
Gerardy, J. [> > > >]
Damas, Jacques mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Département des sciences biomédicales et précliniques >]
Chleide, E. [> > > >]
Lejeune, C. [ > > ]
Decamp, E. [> > > >]
De Tullio, Pascal mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
Delarge, J. [> > > >]
Dresse, Albert mailto [Université de Liège - ULg > Services généraux (Faculté de médecine) > Relations académiques et scientifiques (Médecine) >]
Geczy, J. [> > > >]
1998
Behavioural Pharmacology
Lippincott Williams & Wilkins
9
8
731-7
Yes (verified by ORBi)
International
0955-8810
London
United Kingdom
[en] Animals ; Antidepressive Agents/chemistry/pharmacology ; Blepharoptosis/physiopathology ; Brain/enzymology ; Carbazoles/chemistry/pharmacology ; Female ; Hypothermia/chemically induced/physiopathology ; Mice ; Monoamine Oxidase/metabolism ; Monoamine Oxidase Inhibitors/chemistry/pharmacology ; Rats ; Rats, Wistar ; Reserpine/toxicity ; Stereoisomerism
[en] The interaction with monoamine oxidase A (MAO-A) and B has been shown to be sensitive to the absolute configuration of molecules. Therefore, the aim of this study was to compare the effects of the racemic pirlindole (a selective and reversible MAO-A inhibitor) and its two enantiomers using biochemical techniques (in vitro and ex vivo determination of rat brain MAO-A and MAO-B activity) and behavioural models (forced swimming test and reserpine-induced hypothermia and palpebral ptosis test). In vitro, the MAO-A IC50 of (+/-)-pirlindole, R-(-)-pirlindole and S-(+)-pirlindole were 0.24, 0.43 and 0.18 microM, respectively. Ex vivo, their ID50 were 24.4, 37.8 and 18.7 mg/kg i.p. The differences between the three compounds were not significant, with a ratio between the two enantiomers [R-(-)/S-(+)] of 2.2 in vitro and 2.0 ex vivo. MAO-B was only slightly inhibited. In the forced swimming test and the reserpine-induced hypothermia and ptosis model, the three compounds had an antidepressant profile. In the forced swimming test, the minimal effective dose ratio between the R-(-) and the S-(+) was again around 2.0. The behavioural observations were thus clearly in accordance with the biochemical data.
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/35323

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