The Experts below are selected from a list of 114 Experts worldwide ranked by ideXlab platform

Jesper L Kristensen - One of the best experts on this subject based on the ideXlab platform.

  • A strategic approach to [6,6]-bicyclic lactones: application towards the CD fragment of DHβE
    Beilstein Journal of Organic Chemistry, 2017
    Co-Authors: Tue Heesgaard Jepsen, Francois Crestey, Emil Glibstrup, Anders A Jensen, Jesper L Kristensen
    Abstract:

    We report an effective synthetic protocol to access [6,6]-bicyclic lactone moieties through a regio- and stereoselective intramolecular Mizoroki–Heck cross-coupling reaction followed by a 6π-electrocyclization. This method enabled the first synthesis of the elusive CD fragment of the Erythrina Alkaloid DHβE. Preliminary pharmacological evaluations support the notion that the key pharmacophores of DHβE are located in the A and B rings.

  • design synthesis and biological evaluation of Erythrina Alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists
    Journal of Medicinal Chemistry, 2013
    Co-Authors: Francois Crestey, Morten Borch, Jesper T Andreasen, Jacob Andersen, Thomas Balle, Anders A Jensen, Jesper L Kristensen
    Abstract:

    The synthesis of a new series of Erythrina Alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic Erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The most selective and potent nAChR ligand to come from the series, 6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline (3c) (also a natural product by the name of O-methylcorypalline), displayed submicromolar binding affinity toward the α4β2 nAChR with more than 300-fold selectivity over α4β4, α3β4, and α7. Furthermore, this lead structure (which also has inhibitory activity at monoamine oxidases A and B and at the serotonin and norepinephrine transporters) showed antidepressant-like effect in the mouse forced swim test at 30 mg/kg.

  • Design, Synthesis, and Biological Evaluation of Erythrina Alkaloid Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists
    2013
    Co-Authors: Francois Crestey, Morten Borch, Jacob Andersen, Thomas Balle, Anders A Jensen, Jesper Tobias Andreasen, Jesper L Kristensen
    Abstract:

    The synthesis of a new series of Erythrina Alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic Erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The most selective and potent nAChR ligand to come from the series, 6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline (3c) (also a natural product by the name of O-methylcorypalline), displayed submicromolar binding affinity toward the α4β2 nAChR with more than 300-fold selectivity over α4β4, α3β4, and α7. Furthermore, this lead structure (which also has inhibitory activity at monoamine oxidases A and B and at the serotonin and norepinephrine transporters) showed antidepressant-like effect in the mouse forced swim test at 30 mg/kg

James P. Sullivan - One of the best experts on this subject based on the ideXlab platform.

  • Erysodine, a competitive antagonist at neuronal nicotinic acetylcholine receptors.
    European journal of pharmacology, 1995
    Co-Authors: Michael W. Decker, David J. Anderson, Jorge D. Brioni, Diana L. Donnelly-roberts, Chae Hee Kang, Alyssa B. O'neill, Marietta Piattoni-kaplan, Susan Swanson, James P. Sullivan
    Abstract:

    Erysodine, an Erythrina Alkaloid related to dihydro-beta-erythroidine, was found to be a more potent inhibitor of [3H]cytisine binding at neuronal nicotinic acetylcholine receptors but a less potent inhibitor of [125I]alpha-bungarotoxin binding at muscle-type nicotinic acetylcholine receptors than dihydro-beta-erythroidine. Erysodine was a competitive, reversible antagonist of (-)-nicotine-induced dopamine release from striatal slices and inhibited (-)-nicotine-induced 86Rb+ efflux from IMR-32 cells. Erysodine was equipotent with dihydro-beta-erythroidine in the dopamine release assay but 10-fold more potent in the 86Rb+ efflux assay, suggesting differential subtype selectivity for these two antagonists. Erysodine, systemically administered to mice, entered the brain and significantly attentuated nicotine's hypothermic effects and its anxiolytic-like effects in the elevated plus-maze test. There was greater separation between antagonist and toxic doses for erysodine than for dihydro-beta-erythroidine, perhaps because of erysodine's greater selectivity for neuronal receptors. In rats, erysodine prevented both the early developing decrease and the late-developing increase in locomotor activity produced by (-)-nicotine. The potent and competitive nature of erysodine's antagonism together with its ability to enter the brain after systemic administration suggest that erysodine may be a useful tool in characterizing neuronal nicotinic acetylcholine receptors.

Francois Crestey - One of the best experts on this subject based on the ideXlab platform.

  • A strategic approach to [6,6]-bicyclic lactones: application towards the CD fragment of DHβE
    Beilstein Journal of Organic Chemistry, 2017
    Co-Authors: Tue Heesgaard Jepsen, Francois Crestey, Emil Glibstrup, Anders A Jensen, Jesper L Kristensen
    Abstract:

    We report an effective synthetic protocol to access [6,6]-bicyclic lactone moieties through a regio- and stereoselective intramolecular Mizoroki–Heck cross-coupling reaction followed by a 6π-electrocyclization. This method enabled the first synthesis of the elusive CD fragment of the Erythrina Alkaloid DHβE. Preliminary pharmacological evaluations support the notion that the key pharmacophores of DHβE are located in the A and B rings.

  • design synthesis and biological evaluation of Erythrina Alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists
    Journal of Medicinal Chemistry, 2013
    Co-Authors: Francois Crestey, Morten Borch, Jesper T Andreasen, Jacob Andersen, Thomas Balle, Anders A Jensen, Jesper L Kristensen
    Abstract:

    The synthesis of a new series of Erythrina Alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic Erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The most selective and potent nAChR ligand to come from the series, 6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline (3c) (also a natural product by the name of O-methylcorypalline), displayed submicromolar binding affinity toward the α4β2 nAChR with more than 300-fold selectivity over α4β4, α3β4, and α7. Furthermore, this lead structure (which also has inhibitory activity at monoamine oxidases A and B and at the serotonin and norepinephrine transporters) showed antidepressant-like effect in the mouse forced swim test at 30 mg/kg.

  • Design, Synthesis, and Biological Evaluation of Erythrina Alkaloid Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists
    2013
    Co-Authors: Francois Crestey, Morten Borch, Jacob Andersen, Thomas Balle, Anders A Jensen, Jesper Tobias Andreasen, Jesper L Kristensen
    Abstract:

    The synthesis of a new series of Erythrina Alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic Erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The most selective and potent nAChR ligand to come from the series, 6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline (3c) (also a natural product by the name of O-methylcorypalline), displayed submicromolar binding affinity toward the α4β2 nAChR with more than 300-fold selectivity over α4β4, α3β4, and α7. Furthermore, this lead structure (which also has inhibitory activity at monoamine oxidases A and B and at the serotonin and norepinephrine transporters) showed antidepressant-like effect in the mouse forced swim test at 30 mg/kg

Michael W. Decker - One of the best experts on this subject based on the ideXlab platform.

  • Erysodine, a competitive antagonist at neuronal nicotinic acetylcholine receptors.
    European journal of pharmacology, 1995
    Co-Authors: Michael W. Decker, David J. Anderson, Jorge D. Brioni, Diana L. Donnelly-roberts, Chae Hee Kang, Alyssa B. O'neill, Marietta Piattoni-kaplan, Susan Swanson, James P. Sullivan
    Abstract:

    Erysodine, an Erythrina Alkaloid related to dihydro-beta-erythroidine, was found to be a more potent inhibitor of [3H]cytisine binding at neuronal nicotinic acetylcholine receptors but a less potent inhibitor of [125I]alpha-bungarotoxin binding at muscle-type nicotinic acetylcholine receptors than dihydro-beta-erythroidine. Erysodine was a competitive, reversible antagonist of (-)-nicotine-induced dopamine release from striatal slices and inhibited (-)-nicotine-induced 86Rb+ efflux from IMR-32 cells. Erysodine was equipotent with dihydro-beta-erythroidine in the dopamine release assay but 10-fold more potent in the 86Rb+ efflux assay, suggesting differential subtype selectivity for these two antagonists. Erysodine, systemically administered to mice, entered the brain and significantly attentuated nicotine's hypothermic effects and its anxiolytic-like effects in the elevated plus-maze test. There was greater separation between antagonist and toxic doses for erysodine than for dihydro-beta-erythroidine, perhaps because of erysodine's greater selectivity for neuronal receptors. In rats, erysodine prevented both the early developing decrease and the late-developing increase in locomotor activity produced by (-)-nicotine. The potent and competitive nature of erysodine's antagonism together with its ability to enter the brain after systemic administration suggest that erysodine may be a useful tool in characterizing neuronal nicotinic acetylcholine receptors.

Anders A Jensen - One of the best experts on this subject based on the ideXlab platform.

  • A strategic approach to [6,6]-bicyclic lactones: application towards the CD fragment of DHβE
    Beilstein Journal of Organic Chemistry, 2017
    Co-Authors: Tue Heesgaard Jepsen, Francois Crestey, Emil Glibstrup, Anders A Jensen, Jesper L Kristensen
    Abstract:

    We report an effective synthetic protocol to access [6,6]-bicyclic lactone moieties through a regio- and stereoselective intramolecular Mizoroki–Heck cross-coupling reaction followed by a 6π-electrocyclization. This method enabled the first synthesis of the elusive CD fragment of the Erythrina Alkaloid DHβE. Preliminary pharmacological evaluations support the notion that the key pharmacophores of DHβE are located in the A and B rings.

  • design synthesis and biological evaluation of Erythrina Alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists
    Journal of Medicinal Chemistry, 2013
    Co-Authors: Francois Crestey, Morten Borch, Jesper T Andreasen, Jacob Andersen, Thomas Balle, Anders A Jensen, Jesper L Kristensen
    Abstract:

    The synthesis of a new series of Erythrina Alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic Erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The most selective and potent nAChR ligand to come from the series, 6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline (3c) (also a natural product by the name of O-methylcorypalline), displayed submicromolar binding affinity toward the α4β2 nAChR with more than 300-fold selectivity over α4β4, α3β4, and α7. Furthermore, this lead structure (which also has inhibitory activity at monoamine oxidases A and B and at the serotonin and norepinephrine transporters) showed antidepressant-like effect in the mouse forced swim test at 30 mg/kg.

  • Design, Synthesis, and Biological Evaluation of Erythrina Alkaloid Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists
    2013
    Co-Authors: Francois Crestey, Morten Borch, Jacob Andersen, Thomas Balle, Anders A Jensen, Jesper Tobias Andreasen, Jesper L Kristensen
    Abstract:

    The synthesis of a new series of Erythrina Alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic Erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The most selective and potent nAChR ligand to come from the series, 6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline (3c) (also a natural product by the name of O-methylcorypalline), displayed submicromolar binding affinity toward the α4β2 nAChR with more than 300-fold selectivity over α4β4, α3β4, and α7. Furthermore, this lead structure (which also has inhibitory activity at monoamine oxidases A and B and at the serotonin and norepinephrine transporters) showed antidepressant-like effect in the mouse forced swim test at 30 mg/kg