References of "Damas, Jacques"
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See detailModulation of the Clozapine Structure Increases Its Selectivity for the Dopamine D4 Receptor
Liégeois, Jean-François ULg; Bruhwyler, J.; Damas, Jacques ULg et al

in European Journal of Pharmacology (1995), 273(3), 1-3

Clozapine has a more marked affinity for the recently cloned dopamine D4 receptor than for the dopamine D2 receptor. In the search for a selective ligand for the dopamine D4 receptor, useful as a ... [more ▼]

Clozapine has a more marked affinity for the recently cloned dopamine D4 receptor than for the dopamine D2 receptor. In the search for a selective ligand for the dopamine D4 receptor, useful as a pharmacological tool or as a potent atypical antipsychotic, a pyridobenzodiazepine derivative bioisoster of clozapine, JL 18, 8-methyl-6-(4-methyl-1-piperazinyl)-11H-pyrido [2,3-b][1,4]benzodiazepine, was found to be the most dopamine D4-selective ligand belonging to the diarylazepine class. Indeed, JL 18 binds to the dopamine D4 receptor with affinity up to 25 times superior to that for the dopamine D2 receptor and presents reduced affinities for other receptors. [less ▲]

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See detailPyridobenzoxazepine and Pyridobenzothiazepine Derivatives as Potential Central Nervous System Agents: Synthesis and Neurochemical Study
Liégeois, Jean-François ULg; Rogister, F. A.; Bruhwyler, J. et al

in Journal of Medicinal Chemistry (1994), 37(4), 519-25

In order to characterize the pharmacological profile of the different chemical classes of pyridobenzazepine derivatives, a series of N-methylpiperazinopyrido[1,4]- and -[1,5]- benzoxa- and benzothiazepine ... [more ▼]

In order to characterize the pharmacological profile of the different chemical classes of pyridobenzazepine derivatives, a series of N-methylpiperazinopyrido[1,4]- and -[1,5]- benzoxa- and benzothiazepine derivatives were prepared. The affinities for D2, D1, 5-HT2, and cholinergic (M) receptors were measured. In comparison to dibenzazepine reference compounds, a strong decrease of the affinities was observed, less pronounced, however, for the substituted analogues. Oxazepine and thiazepine analogues like clozapine (except 8-chloro-6-(4-methylpiperazin-1-yl)-pyrido[2,3-b][1,4]benzoxazepin e (9) and 8-chloro-6-(4-methylpiperazin-1-yl)pyrido[2,3-b][1,4]- benzothiazepine (11)) were found to be inactive against apomorphine stereotypies. In the open-field test in rats, different molecules showed a high disinhibitory activity as observed with anxiolytic drugs. Moreover, 8-chloro-5-(4-methylpiperazin-1-yl)pyrido[2,3-b][1,5]benzoxazepine (14) presented a clozapine-like profile that was confirmed in the behavioral model in dogs and showed most of the behavioral characteristics described for antipsychotic drugs. Its neurochemical profile, in particular the 5-HT2/D2 ratio, was also compatible with atypical antipsychotic activity. [less ▲]

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See detailAntiinflammatory activity of Centaurea cyanus flowers
Bodart, Patricia; Damas, Jacques ULg; Goldsztajn, V. et al

in Journal de Pharmacie de Belgique (1994, February), 59(1), 73

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See detailNew Pyridobenzodiazepine Derivatives as Potential Antipsychotics: Synthesis and Neurochemical Study
Liégeois, Jean-François ULg; Bruhwyler, J.; Damas, Jacques ULg et al

in Journal of Medicinal Chemistry (1993), 36(15), 2107-14

The discovery of a new, safe, atypical antipsychotic remains an important challenge. To achieve this goal, a series of N-methylpiperazinopyrido[2,3-b] [1,4]- and -[1,5]- and -pyrido[4,3-b][1,4]- and -[1,5 ... [more ▼]

The discovery of a new, safe, atypical antipsychotic remains an important challenge. To achieve this goal, a series of N-methylpiperazinopyrido[2,3-b] [1,4]- and -[1,5]- and -pyrido[4,3-b][1,4]- and -[1,5]- benzodiazepines were synthesized. The dopaminergic (D1, D2), serotonergic (5-HT2), and cholinergic (M) affinities, frequently remarked in the action mechanisms of antipsychotic drugs, were determined using their respective in vitro receptor binding assays. All affinities were reduced for each compound. Optimal substituents were found to be in the 2- or 8-position for the retention of affinities, while substitution at the 5-position by acyl or alkyl groups dramatically diminished binding affinities. Pyridobenzodiazepine derivatives, such as clozapine, were found to be inactive or only weakly effective against apomorphine-mediated stereotypes in rats. In an original and complex behavioral model developed in dogs and successfully used to differentiate distinct classes of psychotropic drugs and to discriminate between typical and atypical neuroleptic drugs, 8-chloro-6-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b] [1,4]benzodiazepine (9), 8-methyl-6-(4-methyl-1-piperazinyl)-11H-pyrido [2,3-b][1,4]benzodiazepine (12), and 5-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b][1,5]benzodiazepine (16) showed most of the behavioral characteristics previously described for neuroleptics. Their neurochemical profiles, particularly their 5-HT2/D2 pKi ratios, were compatible with an atypical antipsychotic effect. These compounds were selected for further investigation. The proposed modulations could lead to new possibilities for the pharmacochemistry of diarylazepines. [less ▲]

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See detailUn messager intercellulaire original, le NO (monoxyde d'azote)
Liégeois, Jean-François ULg; Damas, Jacques ULg

in Revue Médicale de Liège (1993), 48(7), 406-13

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See detailComparative study of typical neuroleptics, clozapine and newly synthesized clozapine-analogues: correlations between neurochemistry and behaviour.
Bruhwyler, J.; Liégeois, Jean-François ULg; Chleide, E. et al

in Behavioural pharmacology (1992), 3(6), 567-579

While neuroleptic therapy with classical compounds has frequently been associated with extrapyramidal side effects, clozapine has revealed an interesting antipsychotic profile without producing any ... [more ▼]

While neuroleptic therapy with classical compounds has frequently been associated with extrapyramidal side effects, clozapine has revealed an interesting antipsychotic profile without producing any clearcut motor side effects. However, some adverse reactions remained that stimulated the search for improved antipsychotic agents. The aim of this study was to characterize the behavioural and neurochemical profiles of typical neuroleptics (chlorpromazine, haloperidol), clozapine, and four newly synthesized clozapine-analogues. Affinity for dopaminergic (D1,D2), serotonergic (5-HT(2)) and cholinergic (muscarinic) receptors were measured and the ratios of these different binding affinities were determined and correlated with the behavioural effects of the drugs in a complex temporal regulation task in the dog. The four clozapine-analogues showed most of the behavioural characteristics previously described for neuroleptics and their neurochemical profile, particularly their 5-HT(2)/D2 pKi ratio, was compatible with an atypical antipsychotic effect. Among these drugs, JL5 and JL13 showed a high degree of similarity with clozapine. Like clozapine, they did not induce catalepsy and stereotypy/hyperkinesia. Moreover, other motor effects were also reduced (ataxia, akinesia, dystony). and tremor and sialorrhea were completely absent with these two molecules. [less ▲]

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See detailAntiinflammatory Prodelphinidins from Black Currant (Ribes nigrum) Leaves
Tits, Monique ULg; Angenot, Luc ULg; Damas, Jacques ULg et al

in Planta Medica (1991), 57(Supplement issue 2), 134

In a study to select anti-inflammatory medicinal plants, we have observed that extracts of Ribes nigrum significantly inhibited at a dose of 50mg/kg i.p. the carrageenan rat paw edema. We have now proved ... [more ▼]

In a study to select anti-inflammatory medicinal plants, we have observed that extracts of Ribes nigrum significantly inhibited at a dose of 50mg/kg i.p. the carrageenan rat paw edema. We have now proved that the most active fractions contained proanthocyanidins . In the present study, we report on the isolation of three bioactive compounds: two prodelphinidins dimers and a new trimeric one. [less ▲]

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See detailFrom ethnobotanical uses of Strychnos henningsii to antiinflammatories, analgesics and antispasmodics
Tits, Monique ULg; Damas, Jacques ULg; Quetin-Leclercq, Joëlle et al

in Journal of Ethnopharmacology (1991), 34

Strychnos henningsii GILG is used in African traditional medicine for the treatment of various ailments, including rheumatism, gastrointestinal complaints, malaria and snake bites. Different preliminary ... [more ▼]

Strychnos henningsii GILG is used in African traditional medicine for the treatment of various ailments, including rheumatism, gastrointestinal complaints, malaria and snake bites. Different preliminary pharmacological experiments are described. The results show that some of the reported folk medicinal applications of S. henningsii can be at least partially explained by the presence of retuline-like alkaloids, whose use could lead to new antinociceptive (antiinflammatory and analgesic) and antispasmodic drugs. [less ▲]

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See detailUtilisation de composés de la série de la rétuline et de l'isorétuline à titre de composés à activité pharmaceutique, en particulier de médicaments analgésiques, antispasmodiques et antiinflammatoires
Angenot, Luc ULg; Damas, Jacques ULg; Tits, Monique ULg

Patent (1989)

Compounds of retuline series and isoretuline series are described. These alkaloids can be prepared by hemisynthesis from strychnine or strychnobiline that are the main alkaloids of Strychnos nux-vomica ... [more ▼]

Compounds of retuline series and isoretuline series are described. These alkaloids can be prepared by hemisynthesis from strychnine or strychnobiline that are the main alkaloids of Strychnos nux-vomica (strychnine) or Strychnos variabilis (strychnobiline). The compounds of both series (retuline and isoretuline) display antiinflammatory, analgesic and antispasmodic effects that could lead to new medicaments. [less ▲]

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See detailSignification physiopathologique des dosages radioimunologiques des kininogenes humains.
Adam, Albert; Damas, Jacques ULg; Ers, Pierre et al

in Pathologie Biologie (1986), 34(1), 19-24

We quantify total and high molecular weight kininogens by radioimmunoassay. The main characteristic of these molecules is the release of kinins. In this paper we would compare the antigenicity of ... [more ▼]

We quantify total and high molecular weight kininogens by radioimmunoassay. The main characteristic of these molecules is the release of kinins. In this paper we would compare the antigenicity of kininogens with their pharmacological property. [less ▲]

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See detailPlasma prokallikrein and kininogens in burned patients.
Adam, Albert; Damas, Jacques ULg; Albert, Adelin ULg et al

in Thrombosis Research (1986), 41(4), 537-43

Using specific immunological (1) and enzymatic (2) methods, we have measured prokallikrein, total, high, and low molecular weight kininogens in 36 severely burned patients. At admission to the intensive ... [more ▼]

Using specific immunological (1) and enzymatic (2) methods, we have measured prokallikrein, total, high, and low molecular weight kininogens in 36 severely burned patients. At admission to the intensive care unit, all constituents were significantly decreased when compared to previously defined reference intervals. The values remained low during the three first days after burn. The changes affecting total and low molecular weight kininogens were significantly correlated (p less than 0.05) with the severity of the burn area. Prokallikrein and kininogens levels were also closely related to the concentrations of C3c and C4 complement factors. [less ▲]

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See detailHuman kininogens of low and high molecular mass: quantification by radioimmunoassay and determination of reference values.
Adam, Albert; Albert, Adelin ULg; Calay, G et al

in Clinical Chemistry (1985), 31(3), 423-6

Kininogens of low and high molecular mass, highly purified from human plasma, were used to raise antisera in rabbits. To obtain immunologically intact tracers, we labeled the kininogens by the lodogen ... [more ▼]

Kininogens of low and high molecular mass, highly purified from human plasma, were used to raise antisera in rabbits. To obtain immunologically intact tracers, we labeled the kininogens by the lodogen method, followed by double chromatography, first on Sephadex G50 and then on Sephadex G200 for high-molecular-mass kininogen or on G100 for low-molecular-mass kininogen. Both assays are sensitive, accurate, and reproducible. On an equimolar basis, the high-molecular-mass kininogen cross reacted completely in the determination of low-molecular-mass analyte. Moreover, the radioimmunoassay for the former was highly specific. After optimizing the time and temperature of incubation to provide rapid and reliable results, we determined 95% reference intervals from a large sample of healthy subjects (250 men, 200 women): 109-272 and 69-116 mg/L for the low- and high-molecular-mass kininogens, respectively. [less ▲]

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See detailInfluence of oral contraceptives and pregnancy on constituents of the kallikrein-kininogen system in plasma.
Adam, Albert; Albert, Adelin ULg; BOULANGER, Josianne ULg et al

in Clinical Chemistry (1985), 31(9), 1533-6

We measured kininogens of low and high molecular mass along with prokallikrein activity in plasma of women with a normal menstrual cycle. We observed no difference between results for the follicular and ... [more ▼]

We measured kininogens of low and high molecular mass along with prokallikrein activity in plasma of women with a normal menstrual cycle. We observed no difference between results for the follicular and luteal phases. We assayed the same constituents in women who were taking oral contraceptives (combined estroprogestative) and found that activity of prokallikrein and concentrations of low- and high-molecular-mass kininogens were significantly increased. Lastly, we studied the components of the kallikrein-kininogen system during pregnancy. We also observed a marked increase in their concentrations in plasma, despite a decrease in total proteins. Specifically, prokallikrein and kininogens increase continuously with gestational age, reaching their maxima around the eighth month of pregnancy. At that time, more than 50% of observed results fall outside the normal reference interval. Our observations are even more striking when prokallikrein and kininogens are expressed in units per gram of total proteins, to account for the hemodilution. After delivery, the concentrations of prokallikrein and low- and high-molecular-mass kininogens decline promptly, returning to normal within three days. [less ▲]

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See detailSur l'action antioedème de l'escine
Damas, Pierre ULg; Volon, G.; Damas, Jacques ULg et al

in Bulletin de la Société Royale des Sciences de Liège (1976), 9-10

Anti-inflammatory activity of escine. - Escine is one of the most active saponines extracted from Aesculum hippocastanum. As a pure compound, escine-Na inhibits exsudative oedema induced locally in the ... [more ▼]

Anti-inflammatory activity of escine. - Escine is one of the most active saponines extracted from Aesculum hippocastanum. As a pure compound, escine-Na inhibits exsudative oedema induced locally in the rat skin by dextran (MW (0000). This inhibition is due, for a small part, to the release of adrenaline by adrenal medulla; for an other part, to an interaction with glyco-cortico-steroids from the adrenal cortex and, finally, to direct potent vasoconstriction. [less ▲]

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