What question did this study set out to answer?

To review the neurochemical, physiological, and behavioral pharmacology of the partial inverse agonist FG-7142 at the benzodiazepine allosteric site of the GABAA receptor.

December 1, 2007CNS Drug ReviewsOpen Access

Pharmacology of the β‐Carboline FG‐7142, a Partial Inverse Agonist at the Benzodiazepine Allosteric Site of the GABAA Receptor: Neurochemical, Neurophysiological, and Behavioral Effects

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Authors

AEAndrew K. EvansArista (United States)CLChristopher A. LowryUniversity of Colorado Boulder

Discussion

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Implication

Preclinical review demonstrates that partial inverse agonist FG-7142 triggers anxiety and sympathetic reactivity via GABAA receptors, highlighting mechanisms underlying fear circuitry.

Key Points

To review the neurochemical, physiological, and behavioral pharmacology of the partial inverse agonist FG-7142 at the benzodiazepine allosteric site of the GABAA receptor.
Synthesized findings from pharmacological, neurochemical, and behavioral investigations across mammalian and non-mammalian species, including human observations.
Evaluated receptor binding affinities, modulation of GABA-induced chloride flux across GABAA receptor subunits, and interactions with monoaminergic modulatory networks.
FG-7142 exhibits highest binding affinity and efficacy for inhibiting GABA-gated chloride flux at alpha1 subunit-containing GABAA receptors.
Administration activates anxiety-related neural circuits, engaging serotonergic, dopaminergic, cholinergic, and noradrenergic pathways while producing proconflict behaviors, sympathetic acceleration, and neuroendocrine activation.
Acute and chronic dosing induces proconvulsive states, upregulates cortical adrenoreceptors, reduces responsiveness to subsequent GABA agonists, and sensitizes receptors to inverse agonists.

Cite This Study

Evans et al. (2007) studied this question.

synapsesocial.com/papers/6aae3a97c763f45372cc6739 https://doi.org/10.1111/j.1527-3458.2007.00025.x

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Implication

Preclinical review demonstrates that partial inverse agonist FG-7142 triggers anxiety and sympathetic reactivity via GABAA receptors, highlighting mechanisms underlying fear circuitry.

Pharmacology of the β‐Carboline FG‐7142, a Partial Inverse Agonist at the Benzodiazepine Allosteric Site of the GABAA Receptor: Neurochemical, Neurophysiological, and Behavioral Effects

Discussion

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Key Points

Cite This Study

Pharmacology of the β‐Carboline FG‐7142, a Partial Inverse Agonist at the Benzodiazepine Allosteric Site of the GABAA Receptor: Neurochemical, Neurophysiological, and Behavioral Effects

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