3 L2 Drug Types in Neuropharmacology Flashcards
(20 cards)
3 drug targets
Enzymes - Receptors - Transporters
Describe caffiene as an antagonist
Adenosine receptor antagonist
What is the endogenous agonist for adenosine receptors
Adenosine
What kind of G protein subtype are adenosine receptors and what do they do
Gi coupled GPCRs- Decrease intracellular cAMP which can decrease neuron firing
Describe ATP and Adenosine
As ATP is used for energy, it is converted to adenosine - Throughout day, adenosine buildup activates adenosine receptors - Decreases neuron firing and causes us to sleep
Caffeine mechanism of action
Caffeine binds to A1R preventing adenosine from binding and activating R - Increases cAMP and prevents hyper polarisation - Neurons are more likely to depolarise - Decreases inhibotory affect of adenosine, increasing wakefulness
Caffiene in well-rested vs sleep-deprived
Well rested- Improvements in some areas of cognition
Sleep deprived- Larger improvements in aspects of cognition
Caffeine effect in rested state
A1 activity from low to very low (little adenosine)
Caffeine effect in sleep deprived state
A1 activity from high to low (high adenosine available)
Enzyme inhibition mechanism
Enzyme inhibition leads to buildup of endogenous agonists increasing receptor activation
Parkinsons enzyme inhibition
Monoamine oxidase inhibitors
What are protease inhibitors commonly used as
Anti viral drugs
Common side effect of enzyme inhibitors
Many drugs are inhibitors of liver enzymes as an unwanted side effect unrelated to their primary mechanism of action
2 types of transporter drug targets
Inhibitors - Releasing agents
Common transporter inhibitor disease
Psychological diseases
What is the most common type of releasing agent
Amphetamines
Amphetamines mechanism of action
Amphetamines bind to reuptake transporters and vesicle storage proteins - Causes NT buildup in cytoplasm - Transporters reverse and NT accumulate in synapse - High amount of receptor activation
Positive Allosteric Modulators (PAM)
Increase receptor activity when endogenous agonist binds
Describe PAM efficacy with and without agonist
PAM binds without agonist- No efficacy
PAM binds in presence of agonist- Very high efficacy
PAM benefit
Increasing endogenous neurotransmission
