Drugs in CNS Flashcards
Main excitatory neurotransmitter in CNS
Glutamate
Main neurotransmitter in peripheral nervous system
Acetyl choline
Main inhibitory neurotransmitter in CNS
GABA
GABAa receptor share a homology with…
Nicotinic receptors (ligand gated ion channel)
How many proteins make up a GABAa receptor?
5 - pentameric
What is diazapam?
An allosteric modulator of GABAa
What does a positive allosteric modulator do?
Increases affinity for ligand to receptor at orthosteric site- allows for lower conc. of agonist to get same response.
What does an allosteric antagonist do? Is it the same as a negative allosteric modulator?
Allosteric antagonist- binds to allosteric site and prevents effect of negative allosteric regulator
Negative allosteric regulator reduces affinity of orthosteric site
Examples of anxiolytics
Benzodiazapam (agonist), SSRIs (fluoxetine), 5HT,
Benefit of benzodiazapam
Overdose can be treated with a competitive antagonist (flumazenil)
Clinical uses of benzodiazapines
Anticonvulsants, preoperative sedation, anxiolytics
Generalized grand mal seizure symptoms
Both hemispheres of brain have electrical activity, loss of consciousness, generalised continuous high frewuency activiy followed by intermittent discharge
Schizophrenia negative symptoms possible pathogenesis?
Changes in prefrontal cortex
Decreased activation of mesocortical pathway involving D1 receptors
