page_title: GABAA receptor positive allosteric modulator
section_title: Sedation
hierarchical_section_title: GABAA receptor positive allosteric modulator / Applications / Barbiturates / Sedation
caption_attribution_description: English: GABAergic synapse. The synaptic anchoring protein Gephyrin is indirectly linked to the GABAA receptors.
context_page_description: In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system.
  GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present.
  Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation.
  In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. Examples of GABAA PAMs include alcohol, benzodiazepines such as diazepam and alprazolam, Z-drugs such as zolpidem and the barbiturate drugs.
context_section_description: Pentobarbital is used as a hypnotic when analgesia is not required. It´s often used in CT imaging when sedation is needed. It is efficient, safe and the recovery time is short.  In 2013 the barbiturates phenobarbital and butabarbital are still used as sedatives in certain cases as well as to antagonize the effects of drugs as ephedrine and theophylline. Phenobarbital is used in cases of drug withdrawal syndromes. It is used as normal and emergency treatment in some cases of epilepsy.
caption: Fig 4. GABAergic synapse. The synaptic anchoring protein Gephyrin is indirectly linked to the GABAA receptors.
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