The Experts below are selected from a list of 144 Experts worldwide ranked by ideXlab platform
Willy Nerdal - One of the best experts on this subject based on the ideXlab platform.
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Olanzapine interaction with dipalmitoyl phosphatidylcholine (DPPC) and 1-palmitoyl-2-oleoyl phosphatidylserine (POPS) bilayer: a (13)C and (31)P solid-state NMR study.
Biophysical chemistry, 2008Co-Authors: Chen Song, Willy NerdalAbstract:Phospholipid bilayer interaction of olanzapine (OLZ), a thienobenzodiazepine derivative and an antipsychotic agent, has been studied with (13)C and (31)P solid-state NMR. A dipalmitoyl phosphatidylcholine (60%)/1-palmitoyl-2-oleoyl phosphatidylserine (40%) bilayer (DPPC(60%)/POPS(40%)) with 50 wt.% H(2)O, with and without 10 mol% OLZ have been investigated. The results reveal that both the serine and the choline head groups are affected by OLZ interaction with the bilayer. The OLZ interaction with the serine and the choline head groups appears to be caused by electrostatic attraction to the serine head group carboxyl and repulsion of the choline head group positively charged nitrogen. (31)P MAS NMR experiments show the appearance of two new (31)P resonances both for the PS and the PC phosphorous in the presence of OLZ. Static (31)P NMR spectra demonstrate a decrease in chemical shift anisotropy (CSA) of the OLZ containing bilayer when in the liquid-crystalline phase and an increase in CSA when in the gel state.
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Olanzapine interaction with dipalmitoyl phosphatidylcholine (DPPC) and 1-palmitoyl-2-oleoyl phosphatidylserine (POPS) bilayer : A 13C and 31P solid-state NMR study
Biophysical Chemistry, 2008Co-Authors: Chen Song, Willy NerdalAbstract:Phospholipid bilayer interaction of olanzapine (OLZ), a thienobenzodiazepine derivative and an antipsychotic agent, has been studied with (13)C and (31)P solid-state NMR. A dipalmitoyl phosphatidylcholine (60%)/1-palmitoyl-2-oleoyl phosphatidylserine (40%) bilayer (DPPC(60%)/POPS(40%)) with 50 wt.% H(2)O, with and without 10 mol% OLZ have been investigated. The results reveal that both the serine and the choline head groups are affected by OLZ interaction with the bilayer. The OLZ interaction with the serine and the choline head groups appears to be caused by electrostatic attraction to the serine head group carboxyl and repulsion of the choline head group positively charged nitrogen. (31)P MAS NMR experiments show the appearance of two new (31)P resonances both for the PS and the PC phosphorous in the presence of OLZ. Static (31)P NMR spectra demonstrate a decrease in chemical shift anisotropy (CSA) of the OLZ containing bilayer when in the liquid-crystalline phase and an increase in CSA when in the gel state.
Chen Song - One of the best experts on this subject based on the ideXlab platform.
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Olanzapine interaction with dipalmitoyl phosphatidylcholine (DPPC) and 1-palmitoyl-2-oleoyl phosphatidylserine (POPS) bilayer: a (13)C and (31)P solid-state NMR study.
Biophysical chemistry, 2008Co-Authors: Chen Song, Willy NerdalAbstract:Phospholipid bilayer interaction of olanzapine (OLZ), a thienobenzodiazepine derivative and an antipsychotic agent, has been studied with (13)C and (31)P solid-state NMR. A dipalmitoyl phosphatidylcholine (60%)/1-palmitoyl-2-oleoyl phosphatidylserine (40%) bilayer (DPPC(60%)/POPS(40%)) with 50 wt.% H(2)O, with and without 10 mol% OLZ have been investigated. The results reveal that both the serine and the choline head groups are affected by OLZ interaction with the bilayer. The OLZ interaction with the serine and the choline head groups appears to be caused by electrostatic attraction to the serine head group carboxyl and repulsion of the choline head group positively charged nitrogen. (31)P MAS NMR experiments show the appearance of two new (31)P resonances both for the PS and the PC phosphorous in the presence of OLZ. Static (31)P NMR spectra demonstrate a decrease in chemical shift anisotropy (CSA) of the OLZ containing bilayer when in the liquid-crystalline phase and an increase in CSA when in the gel state.
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Olanzapine interaction with dipalmitoyl phosphatidylcholine (DPPC) and 1-palmitoyl-2-oleoyl phosphatidylserine (POPS) bilayer : A 13C and 31P solid-state NMR study
Biophysical Chemistry, 2008Co-Authors: Chen Song, Willy NerdalAbstract:Phospholipid bilayer interaction of olanzapine (OLZ), a thienobenzodiazepine derivative and an antipsychotic agent, has been studied with (13)C and (31)P solid-state NMR. A dipalmitoyl phosphatidylcholine (60%)/1-palmitoyl-2-oleoyl phosphatidylserine (40%) bilayer (DPPC(60%)/POPS(40%)) with 50 wt.% H(2)O, with and without 10 mol% OLZ have been investigated. The results reveal that both the serine and the choline head groups are affected by OLZ interaction with the bilayer. The OLZ interaction with the serine and the choline head groups appears to be caused by electrostatic attraction to the serine head group carboxyl and repulsion of the choline head group positively charged nitrogen. (31)P MAS NMR experiments show the appearance of two new (31)P resonances both for the PS and the PC phosphorous in the presence of OLZ. Static (31)P NMR spectra demonstrate a decrease in chemical shift anisotropy (CSA) of the OLZ containing bilayer when in the liquid-crystalline phase and an increase in CSA when in the gel state.
Somayeh Jafari - One of the best experts on this subject based on the ideXlab platform.
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Novel olanzapine analogues presenting a reduced H_1 receptor affinity and retained 5HT_2A/D_2 binding affinity ratio
BMC Pharmacology, 2012Co-Authors: Somayeh Jafari, Marc E Bouillon, Xu-feng Huang, Stephen G Pyne, Francesca Fernandez-enrightAbstract:Background Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H_1) receptors is believed to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT_2A/D_2) receptor binding affinity ratios. Results We have synthesized novel olanzapine analogues 8a and 8b together with the already known derivative 8c and we have examined their respective in vitro affinities for the 5HT_2A, D_2, and H_1 receptors. Conclusions We suggest that Thienobenzodiazepines 8b and 8c with lower binding affinity for the H_1 receptors, but similar 5HT_2A/D_2 receptor binding affinity ratios to those of olanzapine. These compounds may offer a better pharmacological profile than olanzapine for treating patients with schizophrenia.
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Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects
Journal of neurochemistry, 2011Co-Authors: Somayeh Jafari, Francesca Fernandez-enright, Xu-feng HuangAbstract:Antipsychotic drugs have various neuropharmacological properties as a result of their structural diversity. Despite their therapeutic benefits, most of the prescribed atypical antipsychotics can induce severe side effects, including weight gain, type II diabetes mellitus, and cardiovascular diseases. Among the developed atypical antipsychotic agents, tetracyclic dibenzodiazepine and thienobenzodiazepine compounds, particularly clozapine and olanzapine, are associated with the greatest weight gain and metabolic disturbances. However, the unique chemical structure of these compounds causes the low risk of side effects reported for typical antipsychotics (e.g. extrapyramidal symptoms and tardive dyskinesia). This report reviews the recent discovery of the potential role of the chemical structure of antipsychotics in their therapeutic properties and metabolic disturbances. By developing structure-activity relationship studies for atypical antipsychotics, we will improve our understanding of the structural modifications of these chemical classes that lead to reduced weight gain, which will be an invaluable step toward the discovery of the next generation of atypical antipsychotics. In this review, we suggest that a novel dibenzodiazepine or thienobenzodiazepine antipsychotic drug with lower affinity for H(1) receptors may significantly advance schizophrenia therapy.
Xu-feng Huang - One of the best experts on this subject based on the ideXlab platform.
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Novel olanzapine analogues presenting a reduced H_1 receptor affinity and retained 5HT_2A/D_2 binding affinity ratio
BMC Pharmacology, 2012Co-Authors: Somayeh Jafari, Marc E Bouillon, Xu-feng Huang, Stephen G Pyne, Francesca Fernandez-enrightAbstract:Background Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H_1) receptors is believed to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT_2A/D_2) receptor binding affinity ratios. Results We have synthesized novel olanzapine analogues 8a and 8b together with the already known derivative 8c and we have examined their respective in vitro affinities for the 5HT_2A, D_2, and H_1 receptors. Conclusions We suggest that Thienobenzodiazepines 8b and 8c with lower binding affinity for the H_1 receptors, but similar 5HT_2A/D_2 receptor binding affinity ratios to those of olanzapine. These compounds may offer a better pharmacological profile than olanzapine for treating patients with schizophrenia.
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Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects
Journal of neurochemistry, 2011Co-Authors: Somayeh Jafari, Francesca Fernandez-enright, Xu-feng HuangAbstract:Antipsychotic drugs have various neuropharmacological properties as a result of their structural diversity. Despite their therapeutic benefits, most of the prescribed atypical antipsychotics can induce severe side effects, including weight gain, type II diabetes mellitus, and cardiovascular diseases. Among the developed atypical antipsychotic agents, tetracyclic dibenzodiazepine and thienobenzodiazepine compounds, particularly clozapine and olanzapine, are associated with the greatest weight gain and metabolic disturbances. However, the unique chemical structure of these compounds causes the low risk of side effects reported for typical antipsychotics (e.g. extrapyramidal symptoms and tardive dyskinesia). This report reviews the recent discovery of the potential role of the chemical structure of antipsychotics in their therapeutic properties and metabolic disturbances. By developing structure-activity relationship studies for atypical antipsychotics, we will improve our understanding of the structural modifications of these chemical classes that lead to reduced weight gain, which will be an invaluable step toward the discovery of the next generation of atypical antipsychotics. In this review, we suggest that a novel dibenzodiazepine or thienobenzodiazepine antipsychotic drug with lower affinity for H(1) receptors may significantly advance schizophrenia therapy.
Francesca Fernandez-enright - One of the best experts on this subject based on the ideXlab platform.
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Novel olanzapine analogues presenting a reduced H_1 receptor affinity and retained 5HT_2A/D_2 binding affinity ratio
BMC Pharmacology, 2012Co-Authors: Somayeh Jafari, Marc E Bouillon, Xu-feng Huang, Stephen G Pyne, Francesca Fernandez-enrightAbstract:Background Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H_1) receptors is believed to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT_2A/D_2) receptor binding affinity ratios. Results We have synthesized novel olanzapine analogues 8a and 8b together with the already known derivative 8c and we have examined their respective in vitro affinities for the 5HT_2A, D_2, and H_1 receptors. Conclusions We suggest that Thienobenzodiazepines 8b and 8c with lower binding affinity for the H_1 receptors, but similar 5HT_2A/D_2 receptor binding affinity ratios to those of olanzapine. These compounds may offer a better pharmacological profile than olanzapine for treating patients with schizophrenia.
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Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects
Journal of neurochemistry, 2011Co-Authors: Somayeh Jafari, Francesca Fernandez-enright, Xu-feng HuangAbstract:Antipsychotic drugs have various neuropharmacological properties as a result of their structural diversity. Despite their therapeutic benefits, most of the prescribed atypical antipsychotics can induce severe side effects, including weight gain, type II diabetes mellitus, and cardiovascular diseases. Among the developed atypical antipsychotic agents, tetracyclic dibenzodiazepine and thienobenzodiazepine compounds, particularly clozapine and olanzapine, are associated with the greatest weight gain and metabolic disturbances. However, the unique chemical structure of these compounds causes the low risk of side effects reported for typical antipsychotics (e.g. extrapyramidal symptoms and tardive dyskinesia). This report reviews the recent discovery of the potential role of the chemical structure of antipsychotics in their therapeutic properties and metabolic disturbances. By developing structure-activity relationship studies for atypical antipsychotics, we will improve our understanding of the structural modifications of these chemical classes that lead to reduced weight gain, which will be an invaluable step toward the discovery of the next generation of atypical antipsychotics. In this review, we suggest that a novel dibenzodiazepine or thienobenzodiazepine antipsychotic drug with lower affinity for H(1) receptors may significantly advance schizophrenia therapy.