GABAA Receptor Complex and Sedative-Hypnotic Drugs - pediagenosis
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Wednesday, June 9, 2021

GABAA Receptor Complex and Sedative-Hypnotic Drugs

GABAA Receptor Complex and Sedative-Hypnotic Drugs


GABAA Receptor Complex and Sedative-Hypnotic Drugs

Many CNS depressants, including alcohols, barbiturates, benzo­diazepines, and carbamates, produce sedation (reduction of anxiety) or hypnosis (induction of sleep). Sedative­hypnotics show considerable chemical diversity but share an ability to modulate Cl influx via interaction with the GABAA receptor–Cl channel complex, a heteroligomeric glycoprotein comprising 5 or more membrane­spanning subunits. Various subunit combinations give rise to multiple receptor subtypes. GABA enhances Cl influx by binding to α or β subunits. Cl influx hyperpolarizes the neuron and makes it less likely to fire in response to stimulation (EPSPs). Barbiturates depress neuronal activity by facilitating and prolong­ing inhibitory effects of GABA and Gly by interacting with Cl channel sites and increasing the duration of GABA­mediated channel opening. Benzodiazepines (see Figure 3­9) bind to specific receptor sites on the complex and increase the frequency of GABA­mediated channel opening.


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