GABAergic neurotransmission Flashcards
Why are PAMs useful to augment GABAergic neurotransmission?
The property of the PAM may allow for it to target specific receptor
isoforms (combination of specific subunits), which may be located
only in specific brain regions/neurons.
-This allows for us to target those neurons involved in specific
functions/dysfunction/disorder
What are example PAMs for GABAA receptors?
-Benzodiazepines (very extensive list; anxiolytics, sedatives, hypnotics)
-Barbiturates
-Neuroactive steroids (also called neurosteroids)
What are example PAMs for GABAA receptors?
-Benzodiazepines (very extensive list; anxiolytics, sedatives, hypnotics)
-Barbiturates
-Neuroactive steroids (also called neurosteroids)
what is the Neurosteroids
: Endogenous PAMs and models for new drugs
what is Allopregnanolone
- Allopregnanolone is produced on-demand in response to stress
- Very potent PAM at GABAA receptors
- Provides acute anxiolytic activity
- Further metabolized by hydroxylation
what does GABA stand for
gamma-aminobutyric acid
What types of GABAergic drugs are useful therapeutics?
Positive allosteric modulators
GABA transaminase inhibitor
