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See detailRésolution préparative du pirlindol, journées franco-belges de pharmacochimie
De Tullio, Pascal ULg; Felikidis, A.; Liégeois, Jean-François ULg et al

in Journal de Pharmacie de Belgique (1998), 53

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See detailTentatives de synthèse énantiosélective des isomères R et S du pirlindole
Pirotte, Bernard ULg; De Tullio, Pascal ULg; Stachow, M. et al

in Journal de Pharmacie de Belgique (1998), 53

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See detailPreparative resolution of racemic pirlindole: chromatographic methods and determination of the absolute configuration
De Tullio, Pascal ULg; Ceccato, A.; Liégeois, Jean-François ULg et al

in European Journal of Pharmaceutical Sciences (1998), suppl.1

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See detailRésolution préparative du pirlindole
De Tullio, Pascal ULg; Felekidis, Apostolos ULg; Liégeois, Jean-François ULg et al

in Journal de Pharmacie de Belgique (1998), 53

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See detailJl 13, a Potential Successor to Clozapine, Is Less Sensitive to Oxidative Phenomena
Liégeois, Jean-François ULg; Mouithys-Mickalad, Ange ULg; Bruhwyler, J. et al

in Biochemical and Biophysical Research Communications (1997), 238(1), 252-5

The oxidation behaviour of JL 13, a promising antipsychotic, was investigated in comparison with clozapine and loxapine, by measuring their direct "radical scavenging" abilities and their efficacies in ... [more ▼]

The oxidation behaviour of JL 13, a promising antipsychotic, was investigated in comparison with clozapine and loxapine, by measuring their direct "radical scavenging" abilities and their efficacies in inhibiting the lipid peroxidation. In the lipid peroxidation system, the reactivity of these compounds with free radicals produced by gamma-irradiation of linoleic acid may be presented as follows: JL 13 = loxapine < clozapine. In two enzymatic systems (HRP/GSH and HRP/H2O2/ GSH) which generate the thiyl free radicals, clozapine produces a strong enhancement of the thiyl-radical EPR signal intensity while JL 13 and loxapine exhibit no or minimal effect on this signal. The redox potential values for the three derivatives confirm the spectro-photometric and EPR results. Following this study, we show that JL 13, although presenting a preclinical clozapine-like profile, appears less sensitive to oxidation than clozapine. [less ▲]

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See detailInvolvement of 5-Hydroxytryptamine and Bradykinin in the Hyperalgesia Induced in Rats by Collagenase from Clostridium Histolyticum
Damas, Jacques ULg; Liégeois, Jean-François ULg; Bourdon, V.

in Naunyn-Schmiedeberg's Archives of Pharmacology (1997), 355(5), 566-70

The involvement of bradykinin, 5-hydroxytryptamine, substance P and prostanoids in the hyperalgesia elicited by collagenase in rat paw was investigated. Collagenase (100 micrograms) induced a slight ... [more ▼]

The involvement of bradykinin, 5-hydroxytryptamine, substance P and prostanoids in the hyperalgesia elicited by collagenase in rat paw was investigated. Collagenase (100 micrograms) induced a slight hyperalgesia in kininogen deficient rats in comparison with the behavioural response obtained in normal rats. Lisinopril (10(-5) M), and angiotensin-converting enzyme inhibitor, increased the duration of the hyperalgesia elicited in normal rats. Ondansetron (0.5 to 5 mumol/kg), a 5-HT3 antagonist, suppressed the hyperalgesia as did methysergide (1.1 to 11 mumol/kg), a mixed 5-HT1 and 5-HT2 receptor antagonist. However, the hyperalgesia was not modified by RP 67580 (1.8 to 18 mumol/kg), a NK1 receptor antagonist, and was only slightly delayed by indomethacin (2 mg/kg), a cyclo-oxygenase inhibitor. The oedema-promoting effect of 5-HT (6 nmol) was inhibited by methysergide but not by ondansetron. The swelling induced by collagenase in rat paw was reduced by methysergide but not by ondansetron. We conclude that the behavioural response induced by collagenase depends on an interactions between bradykinin and 5-HT. Prostanoids play a minor role in the beginning of the reaction whereas substance P is not significantly involved in this hyperalgesia. [less ▲]

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See detailTentatives de synthèse énantiosélective des isomères R et S du pirlindole
Pirotte, Bernard ULg; De Tullio, Pascal ULg; Stachow, M. et al

Poster (1997, May)

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See detailLa famille des peptides natriurétiques
Damas, Jacques ULg; Liégeois, Jean-François ULg

in Revue Médicale de Liège (1997), 52(3), 169-73

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See detailDopamine D4 selective ligands as potential antipsychotics
Liégeois, Jean-François ULg; Bruhwyler, J.

in Awouters, Frank (Ed.) Proceedings of the XIVth International Symposium on Medicinal Chemistry (1997)

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See detailJL 13, a pyridobenzoxazepine compound with potential atypical antipsychotic activity: a review of its behavioral properties
Bruhwyler, J.; Liégeois, Jean-François ULg; Bergman, J. et al

in Pharmacological Research (1997), 36

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See detailPirlindole: a selective reversible inhibitor of monoamine oxidase A. A review of its preclinical properties.
Bruhwyler, J.; Liégeois, Jean-François ULg; Geczy, J.

in Pharmacological Research (1997), 36(1), 23-33

Pirlindole is a tetracyclic compound that has been characterized as a potential antidepressant drug. It has pharmacological characteristics in common with both tricyclic antidepressants and classical ... [more ▼]

Pirlindole is a tetracyclic compound that has been characterized as a potential antidepressant drug. It has pharmacological characteristics in common with both tricyclic antidepressants and classical irreversible monoamine oxidase inhibitors. Its main mechanism of action consists of a selective and reversible inhibition of monoamine oxidase A. Secondarily, it exerts an inhibitory effect on noradrenaline and 5-hydroxytryptamine reuptakes. It has no effect on the dopaminergic and cholinergic systems. It has only a low potential for amplifying tyramine and noradrenaline pressor effect, which makes one expect that it will not be at the basis of a 'cheese effect'. Pirlindole has an absolute bioavailability of between 20 and 30% due to an extensive first-pass effect. Orally, the Tmax varies between 2.5 and 6 h in the rat and 0.8 and 2 h in the dog. Two phases of elimination (7.5 and 34-70 h) are measured in the rat and three phases in the dog (1.3, 10.8 and 185 h); it is extensively metabolized. The rat eliminates mainly unconjugated products while the dog eliminates mostly conjugated products. Acute and chronic toxicological studies have not revealed potentially dangerous effects of the drug at the usual doses. It does not present measurable mutagenic, clastogenic or carcinogenic properties. Thus, pirlindole shows pharmacological, pharmacokinetic and toxicological properties which make it suitable for the management of depression. [less ▲]

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See detailPotentiation of the Pro-Inflammatory Effects of Bradykinin by Inhibition of Angiotensin-Converting Enzyme and Aminopeptidase P in Rat Paws
Damas, Jacques ULg; Liégeois, Jean-François ULg; Simmons, W. H.

in Naunyn-Schmiedeberg's Archives of Pharmacology (1996), 354(5), 670-6

The influence of some peptidase inhibitors on oedema and plasma extravasation induced by bradykinin and carrageenan in rat paw was evaluate. Bradykinin-induced oedema in normal rats was increased by o ... [more ▼]

The influence of some peptidase inhibitors on oedema and plasma extravasation induced by bradykinin and carrageenan in rat paw was evaluate. Bradykinin-induced oedema in normal rats was increased by o-phenanthroline (3.10(-2) M), by captopril (10(-6) M to 10(-4) M), by lisinopril (10(-6) M to 10(-4), or by lisinopril (10(-5) M) in combination with apstatin (8.10(-5) M or 1.4 10(-4) M). It was not modified by phosphoramidon (10(-6) M to 10(-5) M) and by diprotin A (10(-3) M). It was increased by mergepta at high concentrations (2.10(-4) M). Mergepta did not increase the potentiating effect of captopril. Carrageenan-oedema in normal rats was increased by captopril (10(-5) M), lisinopril (10(-5) M) and apstatin (1.4 10(-4) M. It was not modified by mergepta (10(-4) M), phosphoramidon (10 (-5) M) and diprotin A (109-3) M). Des-Arg1-bradykinin and Des-Arg9-bradykinin have low oedema-promoting effects. Captopril (10(-5) M) increased the effects of bradykinin but not those of carrageenan in kininogen-deficit Brown Norway rats. Angiotensin-converting enzyme and aminopeptidase P appear to be main kinin-inactivating enzymes in rat paws. Carboxypeptidase N, neutral endopeptidase 24.11 and dipeptidyl(amino)peptidase IV do not play a significant role in this inactivation. [less ▲]

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See detailInfluence of Several Peptidase Inhibitors on the Pro-Inflammatory Effects of Substance P, Capsaicin and Collagenase
Damas, Jacques ULg; Bourdon, V.; Liégeois, Jean-François ULg et al

in Naunyn-Schmiedeberg's Archives of Pharmacology (1996), 354(5), 662-9

Injection of substance P (SP) in a rat hindpaw induced extravasation of 125I-labelled albumin in both hindpaws and salivation. Intravenous injection of SP dose-dependently increased vascular permeability ... [more ▼]

Injection of substance P (SP) in a rat hindpaw induced extravasation of 125I-labelled albumin in both hindpaws and salivation. Intravenous injection of SP dose-dependently increased vascular permeability. This latter effect was increased in rat paws by captopril, an inhibitor of angiotensin-converting enzyme (ACE), administered locally in combination with diprotin A, an inhibitor of an dipeptidyl(amino)peptidase IV (DAP IV) or phosphoramidon, an inhibitor of neutral endopeptidase (NEP). The increase in permeability induced by SP was inhibited by RP 67580, a NK-1-receptor antagonist. Intravenous injection of capsaicin induced labelled albumin extravasation in rat paws. This effect was increased by combination of captopril with diprotin A or phosphoramidon, but not by captopril associated with amastatin, an inhibitor of aminopeptidase M (AmM). It was suppressed by RP 67580. Injection of collagenase in rat paws triggered a swelling and a local plasma exudation. These responses were reduced by RP 67580 but not by RP 68651, its inactive enantiomer. They were increased by combination of captopril with diprotin A or phosphoramidon in normal rats. The potentiating effects of captopril and diprotin A were suppressed by RP 67580 in normal rats but did not develop in kininogen-deficient rats. The oedema induced by collagenase was also increased by lisinopril, another ACE inhibitor, administered locally in combination with apstatin, an inhibitor of aminopeptidase P (AmP). In rats pretreated by methysergide, collagenase-induced oedema was reduced and can be increased by captopril, by lisinopril, administered alone or by lisinopril associated with apstatin. It is concluded that SP is mainly inactivated in rat paws by ACE, DAP IV and NEP. In collagenase-induced oedema, a low amount of SP would be released from afferent nerve terminals by bradykinin formed in low amounts. Bradykinin is inactivated in rat paws by ACE and AmP. In collagenase-oedema, the pro-inflammatory effects of bradykinin are concealed by the effects of the other mediators. [less ▲]

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See detail8-Chloro-5-(4-methylpiperazin-1-yl)-11H-pyrido[2,3-b][1,5]benzodiazepine
Dupont, L.; Liégeois, Jean-François ULg; Rogister, F. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1996), C52

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