05 gaba-extra slide propofol

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How does Propofol cause Hypnotic/Amnesic/Anesthetic Effects? • Propofol is a short‐acting IV‐administered hypnotic/amnesic/anesthetic • Used for induction and maintenance of anesthesia; world’s most highly used IV general anesthetic • Used for short‐term procedural sedation, e.g. endoscopic procedures where fast recovery time is desirable • Potentiates the effect of GABA by increasing GABA affinity and increasing GABA efficacy • Binding site is distinct from GABA and distinct from benzodiazpines. • Binds to the main ligand‐binding subunit (β subunit) in the Pre‐M1 region that is involved in coupling ligand binding in the N terminal extracellular domain to channel opening in the transmembrane pore‐forming domain • Facilitates coupling of GABA binding to channel opening Yip et al, 2013 Propofol

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HowdoesPropofol causeHypnotic/Amnesic/AnestheticEffects?

Propofol isashortactingIVadministeredhypnotic/amnesic/anesthetic

Usedforinductionandmaintenanceofanesthesia;worldsmosthighlyusedIVgeneralanesthetic

Usedforshorttermproceduralsedation,e.g.endoscopicprocedureswherefastrecoverytimeisdesirable

PotentiatestheeffectofGABAbyincreasingGABAaffinityandincreasingGABAefficacy

BindingsiteisdistinctfromGABAanddistinctfrombenzodiazpines.

Bindstothemainligandbindingsubunit( subunit)inthePreM1regionthatisinvolvedincouplingligandbindingintheNterminalextracellulardomaintochannelopeninginthetransmembraneporeformingdomain

FacilitatescouplingofGABAbindingtochannelopening

Yipetal,2013

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