Showing results 141 to 148 of 148
 Anxiolytic potential of sulpiride, clozapine and derivatives in the open-field test.; ; Liégeois, Jean-François  et alin Pharmacology, Biochemistry & Behavior (1990), 36(1), 57-61 Recently acquired data question the sharp dichotomy between anxiolytics and neuroleptics, since disinhibitory effects have been measured in the rat with very low doses of haloperidol and higher doses of ... [more ▼] Recently acquired data question the sharp dichotomy between anxiolytics and neuroleptics, since disinhibitory effects have been measured in the rat with very low doses of haloperidol and higher doses of atypical neuroleptics in FI and DRL schedules, but also in the open-field test. That the DA transmission in certain brain regions is involved in some aspects of anxiety has recently been suggested. The present study confirms this hypothesis particularly with high doses of sulpiride (80 mg/kg) and clozapine (24 mg/kg) when tested in the open-field test. Moreover, the results show how a slight chemical modification of clozapine can give a direction to pharmacological activity with one derivative still resembling clozapine and the second one resembling haloperidol. As neuroleptics do not seem to influence the synthesis and utilization of GABA, the higher entry score observed with them would seem to depend above all on DA antagonism in the mesolimbic system. [less ▲] Detailed reference viewed: 20 (1 ULg)Contribution à l'étude des relations structure-activité parmi les antipsychotiques atypiques : synthèse et évaluation pharmacologique de pyridobenzoazépines bioisostères de la clozapineLiégeois, Jean-François Master of advanced studies dissertation (1990) Detailed reference viewed: 10 (1 ULg)Structure du (Méthyl-1-pipérazinyl-4)-5 Pyrido[2,3-b][1,5]benzothiazépine; ; et al in Acta Crystallographica Section C-Crystal Structure Communications (1988), C44 Detailed reference viewed: 10 (0 ULg)Structure du N-diéthylaminoéthyl méthoxy-4 pyridine sulfonamide-3; ; et al in Acta Crystallographica Section C-Crystal Structure Communications (1988), C44 Detailed reference viewed: 8 (2 ULg)Structure de la clothiapine; ; et al in Acta Crystallographica Section C-Crystal Structure Communications (1987), C43 Detailed reference viewed: 6 (0 ULg)Structure du maléate de (pyrido[2,3-b]benzo-1,5-oxazépinyl-11)-4-méthyl-1H+-pipérazinium, C17H19N4OH + C4H3O4; ; Liégeois, Jean-François et alin Acta Crystallographica Section C-Crystal Structure Communications (1987), C43 Detailed reference viewed: 3 (0 ULg)Structure de l'acide diphénylamino-2 carboxylique; ; et al in Acta Crystallographica Section C-Crystal Structure Communications (1987), C43 Detailed reference viewed: 4 (0 ULg) Analogues of torasemide--structure function relationships--experiments in the thick ascending limb of the loop of Henle of rabbit nephron.; ; et al in Pflügers Archiv : European Journal of Physiology (1987), 408(1), 54-62 The aim of the present study was to examine compounds related to torasemide with respect to their ability to block the equivalent short circuit current, corresponding to the rate of chloride reabsorption ... [more ▼] The aim of the present study was to examine compounds related to torasemide with respect to their ability to block the equivalent short circuit current, corresponding to the rate of chloride reabsorption, in isolated in vitro perfused cortical thick ascending limbs of Henle of the rabbit. The torasemide molecule was modified with respect to the anionic sulfonylurea group, and the secondary amine linked to the pyridine ring. Our results indicate that only few of the tested 48 torasemide-related compounds were able to inhibit from both epithelial sides like torasemide. Only few of the tested compounds were equally effective as torasemide from the lumen side. Some analogues were acting only from the luminal side and some only from the peritubular side. The correlations between structure and potency of inhibition from the luminal side allow the following conclusions: The secondary amine moiety linked to the pyridine ring (toluidine in case of torasemide) can be replaced by a cycloalkylamine or, with some loss of inhibitory potency, by alkylamines. The inhibitory potency is increased with the number of C-atoms in the cycloalkylamine substituted compounds (optimum C7 to C8) and is also depending on the length of the alkylamines (optimum C4). The secondary amine seems to be required since nitrogen cannot be replaced by -S- or -SO2-. The sulfonylurea group cannot be substituted by other anionic groups such as -SO-3 or -COO-. If the pyridine ring is replaced by a NO2-substituted phenyl ring, the inhibitory potency from the luminal side is lost. However, these compounds act still (with some loss of potency) from the peritubular side.(ABSTRACT TRUNCATED AT 250 WORDS) [less ▲] Detailed reference viewed: 15 (4 ULg) |
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