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What type of drugs pass through the BBB?
- Non-polar, lipophilic (lipid soluble)
- Polar, lipophobic usully do not pass
- Exceptions with carrier mediated transport systems; e.g., glucose (protein tyrosine-kinase)
- Abundant in cerebral cortex
- Originates in pyramidal cells of the motor cortex and basal ganglia (both help with motor activities)
- Catecholamines: Dopamine (I) and Norepinephrine (I)
- Serotonin (I)
- Helps regulate motor control; influences moods and emotions
- Has overall excitatory effect d/t disinhibition
- Secreted by neurons in the locus coeruleus of pons
- Mediates inhibition of painful stimuli
- Helps control mood and behavior
- Involved with Renshaw cells
- Main Excitatory NT in CNS
- May be toxic.
- Aspartate is also a excitatory NT
- A peptide the propagates nociception in SC
- Involved in peripheral sensitization (hyperalgesia)
- Excitatory in nature and inhibit painful sensations
- Inhibits enzyme essential for catecholamine (Dopa,Norepi-) synthesis
- Impairs the storage of NT in presynaptic vesicles.
- Antihypertensive drug
MOI: Increase release of catecholamines from presynaptic terminal.
MOI: Impairs release of ACh from presynaptic terminal during AP
MOI: Impair reuptake of NT into presynaptic cleft increasing time in the cleft.
MOI: Inhibits anticholinesterase Keeps ACh in the synapse.
Block postsynaptic receptor
- E.g. Benzodiazepam Diazepam (Valium)
Presynaptic Autoreceptor activation
Serves as a negative feedback to control NT release
Presynaptic Membrane Alteration
Alters the fluidity of membrane to affect release of NT