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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)
: Dopamine (I) and Norepinephrine (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.
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