Modulation of benzodiazepine agonist and inverse-agonist receptor binding by GABA during ethanol withdrawal

Influence of agonist induced internalization on [3H]Ro15‐4513 binding—an application to imaging fluctuations in endogenous GABA with positron emission tomography

“…Some (Verhoeff et al, ), but not all (Frankle et al, ), in vivo imaging studies using GABA A receptor PET ligands have demonstrated that following treatment with these compounds that are known to enhance endogenous GABA the binding of benzodiazepine receptor antagonist radioligands is unaffected and the binding of inverse agonists is altered (Stokes et al, ; Tyacke et al, ). These radioligand‐class specific changes in binding are in agreement with the GABA shift (Kemp et al, ; Maloteaux et al, ; Martin and Candy, ; Mohler and Richards, ; Onoe et al, ; Prather et al, ). However, GABA A receptors are known to endocytose in a clathrin dependent manner on both a constitutive and use dependent basis (Kittler et al, ; Michels and Moss, ).…”

Influence of agonist induced internalization on [3H]Ro15‐4513 binding—an application to imaging fluctuations in endogenous GABA with positron emission tomography

“…Some (Verhoeff et al, ), but not all (Frankle et al, ), in vivo imaging studies using GABA A receptor PET ligands have demonstrated that following treatment with these compounds that are known to enhance endogenous GABA the binding of benzodiazepine receptor antagonist radioligands is unaffected and the binding of inverse agonists is altered (Stokes et al, ; Tyacke et al, ). These radioligand‐class specific changes in binding are in agreement with the GABA shift (Kemp et al, ; Maloteaux et al, ; Martin and Candy, ; Mohler and Richards, ; Onoe et al, ; Prather et al, ). However, GABA A receptors are known to endocytose in a clathrin dependent manner on both a constitutive and use dependent basis (Kittler et al, ; Michels and Moss, ).…”

Animal models of the anxiogenic effects of ethanol withdrawal

“…Mice lacking the γ-2 subunit of GABA A receptor, which is necessary for benzodiazepine sensitivity, show no differences in response to ethanol when compared to normal mice [Homanics et al, 1999]. In addition, the capacity of GABA to modulate receptor affinity for benzodiazepine agonists and inverse-agonists in rat cortex, hippocampus, or cerebellum is not altered during withdrawal from chronic ethanol [Prather et al, 1991a]. Further, GABA B agonists also reverse signs of anxiety during EW [File et al, 1991[File et al, , 1992.…”

Alterations in affective behavior during the time course of alcohol hangover

“…Although the negative hangover effects were announced, the time-extension of them was not assessed. Other research works proposed that anxiogenic responses due to AH may be related to a compensatory alteration in GABA neurotransmission [48] or due to other systems including the brain stress hormone CRF and the neurotransmitter serotonin [49,50].…”

Influence of agonist induced internalization on [3H]Ro15‐4513 binding—an application to imaging fluctuations in endogenous GABA with positron emission tomography

“…Some (Verhoeff et al, ), but not all (Frankle et al, ), in vivo imaging studies using GABA A receptor PET ligands have demonstrated that following treatment with these compounds that are known to enhance endogenous GABA the binding of benzodiazepine receptor antagonist radioligands is unaffected and the binding of inverse agonists is altered (Stokes et al, ; Tyacke et al, ). These radioligand‐class specific changes in binding are in agreement with the GABA shift (Kemp et al, ; Maloteaux et al, ; Martin and Candy, ; Mohler and Richards, ; Onoe et al, ; Prather et al, ). However, GABA A receptors are known to endocytose in a clathrin dependent manner on both a constitutive and use dependent basis (Kittler et al, ; Michels and Moss, ).…”

Animal models of the anxiogenic effects of ethanol withdrawal

“…Mice lacking the γ-2 subunit of GABA A receptor, which is necessary for benzodiazepine sensitivity, show no differences in response to ethanol when compared to normal mice [Homanics et al, 1999]. In addition, the capacity of GABA to modulate receptor affinity for benzodiazepine agonists and inverse-agonists in rat cortex, hippocampus, or cerebellum is not altered during withdrawal from chronic ethanol [Prather et al, 1991a]. Further, GABA B agonists also reverse signs of anxiety during EW [File et al, 1991[File et al, , 1992.…”

Alterations in affective behavior during the time course of alcohol hangover

“…Although the negative hangover effects were announced, the time-extension of them was not assessed. Other research works proposed that anxiogenic responses due to AH may be related to a compensatory alteration in GABA neurotransmission [48] or due to other systems including the brain stress hormone CRF and the neurotransmitter serotonin [49,50].…”

Influence of agonist induced internalization on [3H]Ro15‐4513 binding—an application to imaging fluctuations in endogenous GABA with positron emission tomography

“…Some (Verhoeff et al, ), but not all (Frankle et al, ), in vivo imaging studies using GABA A receptor PET ligands have demonstrated that following treatment with these compounds that are known to enhance endogenous GABA the binding of benzodiazepine receptor antagonist radioligands is unaffected and the binding of inverse agonists is altered (Stokes et al, ; Tyacke et al, ). These radioligand‐class specific changes in binding are in agreement with the GABA shift (Kemp et al, ; Maloteaux et al, ; Martin and Candy, ; Mohler and Richards, ; Onoe et al, ; Prather et al, ). However, GABA A receptors are known to endocytose in a clathrin dependent manner on both a constitutive and use dependent basis (Kittler et al, ; Michels and Moss, ).…”

Animal models of the anxiogenic effects of ethanol withdrawal

“…Mice lacking the γ-2 subunit of GABA A receptor, which is necessary for benzodiazepine sensitivity, show no differences in response to ethanol when compared to normal mice [Homanics et al, 1999]. In addition, the capacity of GABA to modulate receptor affinity for benzodiazepine agonists and inverse-agonists in rat cortex, hippocampus, or cerebellum is not altered during withdrawal from chronic ethanol [Prather et al, 1991a]. Further, GABA B agonists also reverse signs of anxiety during EW [File et al, 1991[File et al, , 1992.…”

Alterations in affective behavior during the time course of alcohol hangover

“…Although the negative hangover effects were announced, the time-extension of them was not assessed. Other research works proposed that anxiogenic responses due to AH may be related to a compensatory alteration in GABA neurotransmission [48] or due to other systems including the brain stress hormone CRF and the neurotransmitter serotonin [49,50].…”