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Roger D. Porsolt - One of the best experts on this subject based on the ideXlab platform.

  • Psychopharmacological profile of a new Chroman Derivative with 5-hydroxytryptamine1A agonist properties: S 20499 (+)
    Drug Development Research, 1992
    Co-Authors: Roger D. Porsolt, Antoine Lenègre, Daniel H. Caignard, Bruno Pfeiffer, Elisabeth Mocaër, Beatrice Guardiola-lemaitre
    Abstract:

    S 20499 is the (+) enantiomer of the racemic compound S 20244 (4-N-(methoxyChromane-3-yl) N-propylamino butyl-8-azaspiro 4,5 decane-7,9 dione), a novel 5-hydroxytryptamine1A (5-HT1A) agonist. The present experiments examined the potential anxiolytic and 5-HT1A agonist activity of S 20499 (+) in behavioral experiments in rodents. Tests used were the lrwin, activity meter, and tail suspension tests in mice and the Vogel conflict, forepaw treading, and lower lip retraction tests in rats. Further tests examined its duration of activity and the effects of chronic treatment. In most experiments, its effects were compared with the (−) enantiomer (S 20500). Neither S 20499 (+) nor S 20500 (−) was lethal in mice up to 256 mg/kg. S 20499 (+) induced signs of sedation (hypoactivity, decreased traction and muscle tone, ptosis, and hypothermia) in the lrwin test in the dose range 4–64 mg/kg i.p. and a dose-dependent decrease in locomotion (activity meter) from 2 mg/kg. At high doses (128–256 mg/kg) S 20500 (−) had qualitatively different effects, inducing signs of excitation and stereotyped behavior. At lower doses (16–64 mg/kg), its effects were similar to those of S 20499 (+) but it was between two- and fourfold less potent. S 20499 (+) increased the duration of immobility in the tail suspension test (anxiolytic/tranquilizing activity) from 16 mg/kg, whereas S 20500 (−) had no effects up to 32 mg/kg. BothS 20499 (+) and S 20500 (−) increased the number of shocks taken in the Vogel conflict test (anxiolytic activity) at 4 and 16 mgikg, respectively. The duration of activity of S 20499 (+) was between 2 and 4 hr and its effects were maintained after chronic administration over 5 days. Finally, both enantiomers induced forepaw treading and lower lip retraction in rats (signs of 5-HT, agonist activity), with S 20499 (+) being at least four times as potent as S 20500 (−). Taken together, the results are consistent with other available data suggesting potential anxiolytic activity for S 20499 (+), probably arising through its agonist activity at central 5-HT1A, receptors. © 1992 Wiley-Liss, Inc.

  • psychopharmacological profile of a new Chroman Derivative with 5 hydroxytryptamine1a agonist properties s 20499
    Drug Development Research, 1992
    Co-Authors: Roger D. Porsolt, Antoine Lenègre, Daniel H. Caignard, Bruno Pfeiffer, Elisabeth Mocaër, Beatrice Guardiolalemaitre
    Abstract:

    S 20499 is the (+) enantiomer of the racemic compound S 20244 (4-N-(methoxyChromane-3-yl) N-propylamino butyl-8-azaspiro 4,5 decane-7,9 dione), a novel 5-hydroxytryptamine1A (5-HT1A) agonist. The present experiments examined the potential anxiolytic and 5-HT1A agonist activity of S 20499 (+) in behavioral experiments in rodents. Tests used were the lrwin, activity meter, and tail suspension tests in mice and the Vogel conflict, forepaw treading, and lower lip retraction tests in rats. Further tests examined its duration of activity and the effects of chronic treatment. In most experiments, its effects were compared with the (−) enantiomer (S 20500). Neither S 20499 (+) nor S 20500 (−) was lethal in mice up to 256 mg/kg. S 20499 (+) induced signs of sedation (hypoactivity, decreased traction and muscle tone, ptosis, and hypothermia) in the lrwin test in the dose range 4–64 mg/kg i.p. and a dose-dependent decrease in locomotion (activity meter) from 2 mg/kg. At high doses (128–256 mg/kg) S 20500 (−) had qualitatively different effects, inducing signs of excitation and stereotyped behavior. At lower doses (16–64 mg/kg), its effects were similar to those of S 20499 (+) but it was between two- and fourfold less potent. S 20499 (+) increased the duration of immobility in the tail suspension test (anxiolytic/tranquilizing activity) from 16 mg/kg, whereas S 20500 (−) had no effects up to 32 mg/kg. BothS 20499 (+) and S 20500 (−) increased the number of shocks taken in the Vogel conflict test (anxiolytic activity) at 4 and 16 mgikg, respectively. The duration of activity of S 20499 (+) was between 2 and 4 hr and its effects were maintained after chronic administration over 5 days. Finally, both enantiomers induced forepaw treading and lower lip retraction in rats (signs of 5-HT, agonist activity), with S 20499 (+) being at least four times as potent as S 20500 (−). Taken together, the results are consistent with other available data suggesting potential anxiolytic activity for S 20499 (+), probably arising through its agonist activity at central 5-HT1A, receptors. © 1992 Wiley-Liss, Inc.

Beatrice Guardiolalemaitre - One of the best experts on this subject based on the ideXlab platform.

  • psychopharmacological profile of a new Chroman Derivative with 5 hydroxytryptamine1a agonist properties s 20499
    Drug Development Research, 1992
    Co-Authors: Roger D. Porsolt, Antoine Lenègre, Daniel H. Caignard, Bruno Pfeiffer, Elisabeth Mocaër, Beatrice Guardiolalemaitre
    Abstract:

    S 20499 is the (+) enantiomer of the racemic compound S 20244 (4-N-(methoxyChromane-3-yl) N-propylamino butyl-8-azaspiro 4,5 decane-7,9 dione), a novel 5-hydroxytryptamine1A (5-HT1A) agonist. The present experiments examined the potential anxiolytic and 5-HT1A agonist activity of S 20499 (+) in behavioral experiments in rodents. Tests used were the lrwin, activity meter, and tail suspension tests in mice and the Vogel conflict, forepaw treading, and lower lip retraction tests in rats. Further tests examined its duration of activity and the effects of chronic treatment. In most experiments, its effects were compared with the (−) enantiomer (S 20500). Neither S 20499 (+) nor S 20500 (−) was lethal in mice up to 256 mg/kg. S 20499 (+) induced signs of sedation (hypoactivity, decreased traction and muscle tone, ptosis, and hypothermia) in the lrwin test in the dose range 4–64 mg/kg i.p. and a dose-dependent decrease in locomotion (activity meter) from 2 mg/kg. At high doses (128–256 mg/kg) S 20500 (−) had qualitatively different effects, inducing signs of excitation and stereotyped behavior. At lower doses (16–64 mg/kg), its effects were similar to those of S 20499 (+) but it was between two- and fourfold less potent. S 20499 (+) increased the duration of immobility in the tail suspension test (anxiolytic/tranquilizing activity) from 16 mg/kg, whereas S 20500 (−) had no effects up to 32 mg/kg. BothS 20499 (+) and S 20500 (−) increased the number of shocks taken in the Vogel conflict test (anxiolytic activity) at 4 and 16 mgikg, respectively. The duration of activity of S 20499 (+) was between 2 and 4 hr and its effects were maintained after chronic administration over 5 days. Finally, both enantiomers induced forepaw treading and lower lip retraction in rats (signs of 5-HT, agonist activity), with S 20499 (+) being at least four times as potent as S 20500 (−). Taken together, the results are consistent with other available data suggesting potential anxiolytic activity for S 20499 (+), probably arising through its agonist activity at central 5-HT1A, receptors. © 1992 Wiley-Liss, Inc.

Beatrice Guardiola-lemaitre - One of the best experts on this subject based on the ideXlab platform.

  • Psychopharmacological profile of a new Chroman Derivative with 5-hydroxytryptamine1A agonist properties: S 20499 (+)
    Drug Development Research, 1992
    Co-Authors: Roger D. Porsolt, Antoine Lenègre, Daniel H. Caignard, Bruno Pfeiffer, Elisabeth Mocaër, Beatrice Guardiola-lemaitre
    Abstract:

    S 20499 is the (+) enantiomer of the racemic compound S 20244 (4-N-(methoxyChromane-3-yl) N-propylamino butyl-8-azaspiro 4,5 decane-7,9 dione), a novel 5-hydroxytryptamine1A (5-HT1A) agonist. The present experiments examined the potential anxiolytic and 5-HT1A agonist activity of S 20499 (+) in behavioral experiments in rodents. Tests used were the lrwin, activity meter, and tail suspension tests in mice and the Vogel conflict, forepaw treading, and lower lip retraction tests in rats. Further tests examined its duration of activity and the effects of chronic treatment. In most experiments, its effects were compared with the (−) enantiomer (S 20500). Neither S 20499 (+) nor S 20500 (−) was lethal in mice up to 256 mg/kg. S 20499 (+) induced signs of sedation (hypoactivity, decreased traction and muscle tone, ptosis, and hypothermia) in the lrwin test in the dose range 4–64 mg/kg i.p. and a dose-dependent decrease in locomotion (activity meter) from 2 mg/kg. At high doses (128–256 mg/kg) S 20500 (−) had qualitatively different effects, inducing signs of excitation and stereotyped behavior. At lower doses (16–64 mg/kg), its effects were similar to those of S 20499 (+) but it was between two- and fourfold less potent. S 20499 (+) increased the duration of immobility in the tail suspension test (anxiolytic/tranquilizing activity) from 16 mg/kg, whereas S 20500 (−) had no effects up to 32 mg/kg. BothS 20499 (+) and S 20500 (−) increased the number of shocks taken in the Vogel conflict test (anxiolytic activity) at 4 and 16 mgikg, respectively. The duration of activity of S 20499 (+) was between 2 and 4 hr and its effects were maintained after chronic administration over 5 days. Finally, both enantiomers induced forepaw treading and lower lip retraction in rats (signs of 5-HT, agonist activity), with S 20499 (+) being at least four times as potent as S 20500 (−). Taken together, the results are consistent with other available data suggesting potential anxiolytic activity for S 20499 (+), probably arising through its agonist activity at central 5-HT1A, receptors. © 1992 Wiley-Liss, Inc.

Pirotte Bernard - One of the best experts on this subject based on the ideXlab platform.

  • N-Aryl-N'-(Chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: Screening, synthesis of simplified Derivatives, and structure-activity relationship analysis
    'Elsevier BV', 2012
    Co-Authors: Goffin Eric, Lamoral-theys Delphine, Tajeddine Nicolas, De Tullio Pascal, Mondin Ludivine, Lefranc Florence, Gailly Philippe, Rogister Bernard, Kiss Robert, Pirotte Bernard
    Abstract:

    A series of Chroman Derivatives previously reported as potassium channel openers, as well as some newly synthesized simplified structures, were examined for their in vitro effects on the growth of three human high-grade glioma cell lines: U373, T98G, and Hs683. Significant in vitro growth inhibitory activity was observed with 2,2-dimethylChroman-type nitro-substituted phenylthioureas, such as compounds 4o and 4p. Interestingly, most tested phenylureas were found to be slightly less active, but more cell selective (normal versus tumor glial cells, such as 3d, 3e, and 3g), thus less toxic, than the corresponding phenylthioureas. No significant differences were observed in terms of Chroman-Derivative-induced growth inhibitory effects between glioma cells sensitive to pro-apoptotic stimuli (Hs683 glioma cells) and glioma cells associated with various levels of resistance to pro-apoptotic stimuli (U373 and T98G glioma cells), a feature that suggests non-apoptotic-mediated growth inhibition. Flow cytometry analyses confirmed the absence of pro-apoptotic effects for phenylthioureas and phenylureas when analyzed in U373 glioma cells and demonstrated U373 cell cycle arrest in the G0/G1 phase. Computer-assisted phase-contrast videomicroscopy revealed that 3d and 3g displayed cytostatic effects, while 3e displayed cytotoxic ones. As a result, this work identified phenylurea-type 2,2-dimethylChromans as a new class of antitumor agents to be further explored for an innovative therapeutic approach for high-grade glioma and/or for a possible new mechanism of action. © 2012 Elsevier Masson SAS. All rights reserved.SCOPUS: ar.jinfo:eu-repo/semantics/publishe

  • N-Aryl-N'-(Chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified Derivatives, and structure-activity relationship analysis.
    2012
    Co-Authors: Goffin Eric, Lamoral-theys Delphine, Tajeddine Nicolas, De Tullio Pascal, Mondin Ludivine, Lefranc Florence, Gailly Philippe, Rogister Bernard, Kiss Robert, Pirotte Bernard
    Abstract:

    A series of Chroman Derivatives previously reported as potassium channel openers, as well as some newly synthesized simplified structures, were examined for their in vitro effects on the growth of three human high-grade glioma cell lines: U373, T98G, and Hs683. Significant in vitro growth inhibitory activity was observed with 2,2-dimethylChroman-type nitro-substituted phenylthioureas, such as compounds 4o and 4p. Interestingly, most tested phenylureas were found to be slightly less active, but more cell selective (normal versus tumor glial cells, such as 3d, 3e, and 3g), thus less toxic, than the corresponding phenylthioureas. No significant differences were observed in terms of Chroman-Derivative-induced growth inhibitory effects between glioma cells sensitive to pro-apoptotic stimuli (Hs683 glioma cells) and glioma cells associated with various levels of resistance to pro-apoptotic stimuli (U373 and T98G glioma cells), a feature that suggests non-apoptotic-mediated growth inhibition. Flow cytometry analyses confirmed the absence of pro-apoptotic effects for phenylthioureas and phenylureas when analyzed in U373 glioma cells and demonstrated U373 cell cycle arrest in the G0/G1 phase. Computer-assisted phase-contrast videomicroscopy revealed that 3d and 3g displayed cytostatic effects, while 3e displayed cytotoxic ones. As a result, this work identified phenylurea-type 2,2-dimethylChromans as a new class of antitumor agents to be further explored for an innovative therapeutic approach for high-grade glioma and/or for a possible new mechanism of action.Peer reviewe

Bruno Pfeiffer - One of the best experts on this subject based on the ideXlab platform.

  • Psychopharmacological profile of a new Chroman Derivative with 5-hydroxytryptamine1A agonist properties: S 20499 (+)
    Drug Development Research, 1992
    Co-Authors: Roger D. Porsolt, Antoine Lenègre, Daniel H. Caignard, Bruno Pfeiffer, Elisabeth Mocaër, Beatrice Guardiola-lemaitre
    Abstract:

    S 20499 is the (+) enantiomer of the racemic compound S 20244 (4-N-(methoxyChromane-3-yl) N-propylamino butyl-8-azaspiro 4,5 decane-7,9 dione), a novel 5-hydroxytryptamine1A (5-HT1A) agonist. The present experiments examined the potential anxiolytic and 5-HT1A agonist activity of S 20499 (+) in behavioral experiments in rodents. Tests used were the lrwin, activity meter, and tail suspension tests in mice and the Vogel conflict, forepaw treading, and lower lip retraction tests in rats. Further tests examined its duration of activity and the effects of chronic treatment. In most experiments, its effects were compared with the (−) enantiomer (S 20500). Neither S 20499 (+) nor S 20500 (−) was lethal in mice up to 256 mg/kg. S 20499 (+) induced signs of sedation (hypoactivity, decreased traction and muscle tone, ptosis, and hypothermia) in the lrwin test in the dose range 4–64 mg/kg i.p. and a dose-dependent decrease in locomotion (activity meter) from 2 mg/kg. At high doses (128–256 mg/kg) S 20500 (−) had qualitatively different effects, inducing signs of excitation and stereotyped behavior. At lower doses (16–64 mg/kg), its effects were similar to those of S 20499 (+) but it was between two- and fourfold less potent. S 20499 (+) increased the duration of immobility in the tail suspension test (anxiolytic/tranquilizing activity) from 16 mg/kg, whereas S 20500 (−) had no effects up to 32 mg/kg. BothS 20499 (+) and S 20500 (−) increased the number of shocks taken in the Vogel conflict test (anxiolytic activity) at 4 and 16 mgikg, respectively. The duration of activity of S 20499 (+) was between 2 and 4 hr and its effects were maintained after chronic administration over 5 days. Finally, both enantiomers induced forepaw treading and lower lip retraction in rats (signs of 5-HT, agonist activity), with S 20499 (+) being at least four times as potent as S 20500 (−). Taken together, the results are consistent with other available data suggesting potential anxiolytic activity for S 20499 (+), probably arising through its agonist activity at central 5-HT1A, receptors. © 1992 Wiley-Liss, Inc.

  • psychopharmacological profile of a new Chroman Derivative with 5 hydroxytryptamine1a agonist properties s 20499
    Drug Development Research, 1992
    Co-Authors: Roger D. Porsolt, Antoine Lenègre, Daniel H. Caignard, Bruno Pfeiffer, Elisabeth Mocaër, Beatrice Guardiolalemaitre
    Abstract:

    S 20499 is the (+) enantiomer of the racemic compound S 20244 (4-N-(methoxyChromane-3-yl) N-propylamino butyl-8-azaspiro 4,5 decane-7,9 dione), a novel 5-hydroxytryptamine1A (5-HT1A) agonist. The present experiments examined the potential anxiolytic and 5-HT1A agonist activity of S 20499 (+) in behavioral experiments in rodents. Tests used were the lrwin, activity meter, and tail suspension tests in mice and the Vogel conflict, forepaw treading, and lower lip retraction tests in rats. Further tests examined its duration of activity and the effects of chronic treatment. In most experiments, its effects were compared with the (−) enantiomer (S 20500). Neither S 20499 (+) nor S 20500 (−) was lethal in mice up to 256 mg/kg. S 20499 (+) induced signs of sedation (hypoactivity, decreased traction and muscle tone, ptosis, and hypothermia) in the lrwin test in the dose range 4–64 mg/kg i.p. and a dose-dependent decrease in locomotion (activity meter) from 2 mg/kg. At high doses (128–256 mg/kg) S 20500 (−) had qualitatively different effects, inducing signs of excitation and stereotyped behavior. At lower doses (16–64 mg/kg), its effects were similar to those of S 20499 (+) but it was between two- and fourfold less potent. S 20499 (+) increased the duration of immobility in the tail suspension test (anxiolytic/tranquilizing activity) from 16 mg/kg, whereas S 20500 (−) had no effects up to 32 mg/kg. BothS 20499 (+) and S 20500 (−) increased the number of shocks taken in the Vogel conflict test (anxiolytic activity) at 4 and 16 mgikg, respectively. The duration of activity of S 20499 (+) was between 2 and 4 hr and its effects were maintained after chronic administration over 5 days. Finally, both enantiomers induced forepaw treading and lower lip retraction in rats (signs of 5-HT, agonist activity), with S 20499 (+) being at least four times as potent as S 20500 (−). Taken together, the results are consistent with other available data suggesting potential anxiolytic activity for S 20499 (+), probably arising through its agonist activity at central 5-HT1A, receptors. © 1992 Wiley-Liss, Inc.