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78 Cards in this Set

  • Front
  • Back
AP
-depend on Na+/K+ channels
-electrical along nerve
NT
Chemical at nerve ending
Response=
Transmitter + Receptor
CNS acts on which 3 systems?
-Peripheral
-Autonomic
-Somatic
NT for sympathetic NS ?
Noradrenaline
Norad acts on
Alpha & Beta receptors
Parasympathetic NS uses
ACh as NT(pupil constriction and Increased salivation)
Ach acts on
Muscarinic receptors.
NT for somatic system?
ACh--> acts on Nicotinic receptors(MUSCLES)
Some drugs that affect PNS can have
Dramatic CNS effects
Receptors important for
Transmitter recognition & signal transduction.
Ion channels important for
AP propagation and NT release
Enzymes
Transmitter synthesis/inactivation
Transporters
Transmitter synthesis/inactivation.
Steps common in both CNS & PNS where drugs can act ?
-Synthesis,storage,release & inactivation of NT,activation of receptors on target tissue.
Cerebral cortex
-Abstract thought
-memory
-Consciousness
Mesencephalon
-Emotion
-Motivation
-motor coordination,memory
Cerebellum
-Mvt and posture
Brainstem
Reflex co-ordination of CV and respiratory systems
Spinal cord
afferent and efferent neural connection to periphery.
Peripheral NT
ACh & NORAD.
Monoamines NTs
Adrenaline,Dopamine,Serotonin
Amino acids NTs
GABA & glutamate
Peptides NT
Opioids
Small molecules NT
Nitric oxide
How are drugs that INCREASE Norad and Serotonin levels called?
Antidepressants
In the tx of Parkinson's disease,we use drugs that
Increase dopamine in basal ganglia(need to balance with Increased dopamine in other areas of brain-schizo/drug dependence)
In the tx of EPILEPSY,we use drugs that
Increase GABA activity in brain
Drugs that inhibit muscarinic ACh receptors
are use to treat some of the symptoms of Parkinson's/
Potential use of drugs that increase ACh levels in tx of
Alzheimer's disease.
Centrally acting drugs are generally assoc. with
numerous side effects.
Dopamine D2 receptor function in
Schizo.
Chemical signalling is not only important for communication of info between neurones but also for their
Survival
Neurotrophic factors
-maintain neuronal integrity/vital for nerve function
-loss of factors leads to nerve cell degeneration.
Norad. pathway
Tyrosine-->L-DOPA-->Dopamine-->Norad.
What is the max. V1 enz. in the above pathway?
Tyrosine hydroxylase
Dopa carboxylase acts
On L-DOPA --> dopamine
Dopamine is taken up by
vesicles(previous steps in the pathway takes place in cytoplasm)
Where does the rn. involving dopamine takes place?
Inside vesicles--> dopamine Beta hydroxylase--> Noradrenaline
Tyrosine hydroxylase acts on
tyrosine--> L-DOPA
Amphetamine displaces
NA from vesicles(wakefulness but psychoses)
L-DOPA
for Parkinson's pts
"Reserpin"
Lost libido /erectile dysfunction.
Norad. inactivation
Uptake followed by metabolism
2 types of uptake of NA occurs:-
-Neuronal uptake
-Extra neuronal uptake
2 enz. involved in metabolism of NA :-
-COMT
-MAO
Drug interfering with neuronal uptake of NA
Cocaine
Drug interfering with metabolism of NA
Moclobemide
Both drugs above can affect
Mood.
NA affect
-Mood
-BP
ACh affect
-Memory
-Learning
-Motor function
Depression assoc. with
Falls in Norad.,Dopamine,Serotonin in brain.
Inhibition of uptake
Elevates mood.
Cocaine blocks
Serotonin & dopamine uptake
Dopamine assoc. with
Dependence and psychoses.
SSRIs
Selective Serotonin Uptake Inhibitors
SSRIs
Effective Antidepressants.
Serotonin causes
Psychoses + hallucinations.
Monoamine oxidase inhibition
Elevates mood.
Monoamine oxidase A
Norad. is preferred susbtrate
Monoamine oxidase A INHIBITORS used for
depression
Monoamine oxidase B
Dopamine is preferred substrate for metabolism.
Monoamine oxidase B INHIBITORS used for
Parkinson's.
By interfering with synthesis and inactivation,
Reduced specificity.
Transmitter-receptor interaction provides
Greatest specificity.(existence of receptor subtypes-D1/D2 receptors)
For greater specificity,we target
Receptor subtype.
Receptor types
-Ligand gated
-G-protein coupled
-Tyrosine kinase
-Cytoplasmic/nuclear
Ligand gated receptors
-Use Ions/Ca2+ conc. change
-Milliseconds
G-protein coupled receptors
-Muscarinic
-Alpha & Beta adrenoceptors
-Second messengers
-Ca2+ release
-Protein phosphorylation
-Seconds
Tyrosine kinase receptors
-Second messengers
-Minutes
Cytoplasmic/nuclear receptors
-mRNA synthesis
-pz synthesis
-Hours
Pre synaptic input to neurones :-
-nerve terminals
-Modulation of release(autoreceptors such as NT/heteroreceptors-1 nerve regulating release of another one)
Post-synaptic input to neurones
-Cell body/dendrites
-AP generation.
Epilepsy
Excessive discharge of motor nerves
Rx to treat epilepsy
-Reduce excitatory input
-Enhance inhibitory input
GABA
inhibitory
Glutamate
Excitatory
Phenytoin
Limits excitatory nerve activation-stops firing of AP