The Experts below are selected from a list of 201 Experts worldwide ranked by ideXlab platform
Phil Skolnick - One of the best experts on this subject based on the ideXlab platform.
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Volatile anesthetics bidirectionally and stereospecifically modulate ligand binding to GABA Receptors
European journal of pharmacology, 1994Co-Authors: Bradford D. Harris, Anthony S. Basile, Eric J. Moody, Phil SkolnickAbstract:Pharmacologically relevant concentrations of volatile anesthetics can bidirectionally modulate radioligand binding to GABAA Receptors. In mouse cerebral cortex, halothane (a prototypic volatile anesthetic) increased [3H]muscimol (a GABA Receptor agonist) binding while inhibiting the binding of a GABA Receptor Antagonist ([3H]SR 95531). These bidirectional effects of inhalational anesthetics on ligand binding to GABA Receptors are effected through changes in the Bmax with no significant alterations in the KD of these radioligands. Moreover, the concentration dependent, bidirectional modulation of radioligand binding to GABA Receptors by volatile anesthetics exhibited stereoselectivity. Thus, (+)-isoflurane was about twice as potent as the (-)-enantiomer in enhancing [3H]muscimol binding and approximately 50% more potent as an inhibitor of [3H]SR 95531 binding, respectively. The demonstration of a bidirectional, stereospecific modulation of radioligand binding to GABA Receptors by inhalational agents is consistent with the presence of specific recognition sites for inhalational anesthetics on the GABAA Receptor complex.
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Volatile anesthetics bidirectionally and stereospecifically modulate ligand binding to GABA Receptors
European journal of pharmacology, 1994Co-Authors: Bradford D. Harris, Anthony S. Basile, Eric J. Moody, Phil SkolnickAbstract:Pharmacologically relevant concentrations of volatile anesthetics can bidirectionally modulate radioligand binding to GABAA Receptors. In mouse cerebral cortex, halothane (a prototypic volatile anesthetic) increased [3H]muscimol (a GABA Receptor agonist) binding while inhibiting the binding of a GABA Receptor Antagonist ([3H]SR 95531). These bidirectional effects of inhalational anesthetics on ligand binding to GABA Receptors are effected through changes in the Bmax with no significant alterations in the KD of these radioligands. Moreover, the concentration dependent, bidirectional modulation of radioligand binding to GABA Receptors by volatile anesthetics exhibited stereoselectivity. Thus, (+)-isoflurance was about twice as potent as the (−)-enantiomer in enhancing [3H]muscimol binding and ∼50% more potent as an inhibitor of [3H]SR 95531 binding, respectively. The demonstration of a bidirectional, stereospecific modulation of radioligand binding to GABA Receptors by inhalational agents is consistent with the presence of specific recognition sites for inhalational anesthetics on the GABAA Receptor complex.
R J Walker - One of the best experts on this subject based on the ideXlab platform.
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An ion-sensitive microelectrode study on the effect of a high concentration of ivermectin on chloride balance in the somatic muscle bag cells of Ascaris suum.
Parasitology, 1993Co-Authors: H R Parri, M B Djamgoz, L Holden-dye, R J WalkerAbstract:Ivermectin has been shown to increase chloride conductances of invertebrate cells. On the muscle cells of the parasitic nematode Ascaris, ivermectin acts as both a GABA Receptor Antagonist and a chloride channel opener. In this study, ion-sensitive microelectrodes were used to investigate the effect of ivermectin on intracellular Cl- concentration of the somatic muscle bag cells of Ascaris suum. Incubation of muscle cells with ivermectin (10 microM in 1% dimethyl sulphoxide vehicle for 60 min) increased intracellular Cl- by 2.9 mM or 15% compared to controls (P < 0.01, n = 6).
Bradford D. Harris - One of the best experts on this subject based on the ideXlab platform.
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Volatile anesthetics bidirectionally and stereospecifically modulate ligand binding to GABA Receptors
European journal of pharmacology, 1994Co-Authors: Bradford D. Harris, Anthony S. Basile, Eric J. Moody, Phil SkolnickAbstract:Pharmacologically relevant concentrations of volatile anesthetics can bidirectionally modulate radioligand binding to GABAA Receptors. In mouse cerebral cortex, halothane (a prototypic volatile anesthetic) increased [3H]muscimol (a GABA Receptor agonist) binding while inhibiting the binding of a GABA Receptor Antagonist ([3H]SR 95531). These bidirectional effects of inhalational anesthetics on ligand binding to GABA Receptors are effected through changes in the Bmax with no significant alterations in the KD of these radioligands. Moreover, the concentration dependent, bidirectional modulation of radioligand binding to GABA Receptors by volatile anesthetics exhibited stereoselectivity. Thus, (+)-isoflurane was about twice as potent as the (-)-enantiomer in enhancing [3H]muscimol binding and approximately 50% more potent as an inhibitor of [3H]SR 95531 binding, respectively. The demonstration of a bidirectional, stereospecific modulation of radioligand binding to GABA Receptors by inhalational agents is consistent with the presence of specific recognition sites for inhalational anesthetics on the GABAA Receptor complex.
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Volatile anesthetics bidirectionally and stereospecifically modulate ligand binding to GABA Receptors
European journal of pharmacology, 1994Co-Authors: Bradford D. Harris, Anthony S. Basile, Eric J. Moody, Phil SkolnickAbstract:Pharmacologically relevant concentrations of volatile anesthetics can bidirectionally modulate radioligand binding to GABAA Receptors. In mouse cerebral cortex, halothane (a prototypic volatile anesthetic) increased [3H]muscimol (a GABA Receptor agonist) binding while inhibiting the binding of a GABA Receptor Antagonist ([3H]SR 95531). These bidirectional effects of inhalational anesthetics on ligand binding to GABA Receptors are effected through changes in the Bmax with no significant alterations in the KD of these radioligands. Moreover, the concentration dependent, bidirectional modulation of radioligand binding to GABA Receptors by volatile anesthetics exhibited stereoselectivity. Thus, (+)-isoflurance was about twice as potent as the (−)-enantiomer in enhancing [3H]muscimol binding and ∼50% more potent as an inhibitor of [3H]SR 95531 binding, respectively. The demonstration of a bidirectional, stereospecific modulation of radioligand binding to GABA Receptors by inhalational agents is consistent with the presence of specific recognition sites for inhalational anesthetics on the GABAA Receptor complex.
H R Parri - One of the best experts on this subject based on the ideXlab platform.
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An ion-sensitive microelectrode study on the effect of a high concentration of ivermectin on chloride balance in the somatic muscle bag cells of Ascaris suum.
Parasitology, 1993Co-Authors: H R Parri, M B Djamgoz, L Holden-dye, R J WalkerAbstract:Ivermectin has been shown to increase chloride conductances of invertebrate cells. On the muscle cells of the parasitic nematode Ascaris, ivermectin acts as both a GABA Receptor Antagonist and a chloride channel opener. In this study, ion-sensitive microelectrodes were used to investigate the effect of ivermectin on intracellular Cl- concentration of the somatic muscle bag cells of Ascaris suum. Incubation of muscle cells with ivermectin (10 microM in 1% dimethyl sulphoxide vehicle for 60 min) increased intracellular Cl- by 2.9 mM or 15% compared to controls (P < 0.01, n = 6).
Lin Chen - One of the best experts on this subject based on the ideXlab platform.
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sodium salicylate suppresses GABAergic inhibitory activity in neurons of rodent dorsal raphe nucleus
PLOS ONE, 2015Co-Authors: Yan Jin, Bin Luo, Xin Xing Wang, Liang Chen, Ming Wang, Wei Wen Wang, Lin ChenAbstract:Sodium salicylate (NaSal), a tinnitus inducing agent, can activate serotonergic (5-HTergic) neurons in the dorsal raphe nucleus (DRN) and can increase serotonin (5-HT) level in the inferior colliculus and the auditory cortex in rodents. To explore the underlying neural mechanisms, we first examined effects of NaSal on neuronal intrinsic properties and the inhibitory synaptic transmissions in DRN slices of rats by using whole-cell patch-clamp technique. We found that NaSal hyperpolarized the resting membrane potential, decreased the input resistance, and suppressed spontaneous and current-evoked firing in GABAergic neurons, but not in 5-HTergic neurons. In addition, NaSal reduced GABAergic spontaneous and miniature inhibitory postsynaptic currents in 5-HTergic neurons. We next examined whether the observed depression of GABAergic activity would cause an increase in the excitability of 5-HTergic neurons using optogenetic technique in DRN slices of the transgenic mouse with channelrhodopsin-2 expressed in GABAergic neurons. When the GABAergic inhibition was enhanced by optical stimulation to GABAergic neurons in mouse DRN, NaSal significantly depolarized the resting membrane potential, increased the input resistance and increased current-evoked firing of 5-HTergic neurons. However, NaSal would fail to increase the excitability of 5-HTergic neurons when the GABAergic synaptic transmission was blocked by picrotoxin, a GABA Receptor Antagonist. Our results indicate that NaSal suppresses the GABAergic activities to raise the excitability of local 5-HTergic neural circuits in the DRN, which may contribute to the elevated 5-HT level by NaSal in the brain.
