neurons & neural transmission neurochemical mechanisms of drug action
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NEURONSNEURONS&&
NEURAL TRANSMISSIONNEURAL TRANSMISSION
NEUROCHEMICAL MECHANISMS OF NEUROCHEMICAL MECHANISMS OF DRUG ACTIONDRUG ACTION
Nervous System DivisionsNervous System Divisions CNS (central nervous CNS (central nervous
system)system) Brain, Spinal Cord Brain, Spinal Cord 12 pairs of cranial nerves 12 pairs of cranial nerves
(originate from cranium)(originate from cranium)
PNS (peripheral nervous PNS (peripheral nervous system)system) Somatic nervous systemSomatic nervous system
• 31 pairs of spinal nerves31 pairs of spinal nerves Autonomic nervous systemAutonomic nervous system
CNS ORGANIZATIONCNS ORGANIZATION
Autonomic Nervous SystemAutonomic Nervous System
NEURONSNEURONS
NEURON MEMBRANENEURON MEMBRANE
Membrane StructureMembrane Structure Semipermeable lipid Semipermeable lipid
bilayerbilayer ProteinsProteins
• Ion channelsIon channels• Transport pumpsTransport pumps• ReceptorsReceptors
MEMBRANE POTENTIALMEMBRANE POTENTIAL
ACTION POTENTIALACTION POTENTIAL
ACTION POTENTIALACTION POTENTIAL
CONDUCTION OF A.P.CONDUCTION OF A.P.
NEURONAL COMMUNICATIONNEURONAL COMMUNICATION
POSTSYNAPTIC POSTSYNAPTIC POTENTIALSPOTENTIALS Excitatory PSPExcitatory PSP Inhibitory PSPInhibitory PSP
NEUROCHEMICAL SYNAPSENEUROCHEMICAL SYNAPSE
Presynaptic Presynaptic MembraneMembrane
Postsynaptic Postsynaptic MembraneMembrane
Synaptic VesiclesSynaptic Vesicles Synaptic CleftSynaptic Cleft Receptor SitesReceptor Sites
SYNAPTIC TRANSMISSIONSYNAPTIC TRANSMISSION SynthesisSynthesis StorageStorage Neurotransmitter Neurotransmitter
ReleaseRelease Receptor ActivationReceptor Activation Neurotransmitter Neurotransmitter
DeactivationDeactivation Enzymatic Deactivation Enzymatic Deactivation
(Metabolism)(Metabolism) ReuptakeReuptake
SYNTHESISSYNTHESIS
NEUROTRANSMITTER FAMILIESNEUROTRANSMITTER FAMILIES AcetylcholineAcetylcholine MonoaminesMonoamines
NorepinephrineNorepinephrine DopamineDopamine SerotoninSerotonin
Amino Acid TransmittersAmino Acid Transmitters GlutamateGlutamate GABAGABA HistamineHistamine GlycineGlycine
NeuropeptidesNeuropeptides EnkephalinsEnkephalins EndorphinsEndorphins
Receptor Subtypes for Receptor Subtypes for NeurotransmittersNeurotransmitters
Acetylcholine: nicotinic, muscarinicAcetylcholine: nicotinic, muscarinic Dopamine: D1, D2, D3, D4, D5Dopamine: D1, D2, D3, D4, D5 Norepinephrine: alphaNorepinephrine: alpha11, alpha, alpha22, beta, beta11, beta, beta22
Serotonin: 5-HTSerotonin: 5-HT1a,1b,1c,1d1a,1b,1c,1d; 5-HT; 5-HT2a,2b,2c;2a,2b,2c;; 5-HT; 5-HT3…3…
GABA: GABAGABA: GABAAA, GABA, GABABB
Glutamate: NMDA, AMPA, mGluRGlutamate: NMDA, AMPA, mGluR Endorphins: mu, kappa, deltaEndorphins: mu, kappa, delta
NEUROCHEMICAL PATHWAYSNEUROCHEMICAL PATHWAYS
RECEPTOR ACTIVATIONRECEPTOR ACTIVATION Ligand-gated ion channelsLigand-gated ion channels Ionotropic ReceptorsIonotropic Receptors Metabotropic ReceptorsMetabotropic Receptors
G proteinsG proteins Second MessengersSecond Messengers
RECEPTOR ACTIVATIONRECEPTOR ACTIVATION
DRUG ACTIONS ON RECEPTOR DRUG ACTIONS ON RECEPTOR ACTIVATIONACTIVATION
AgonistsAgonists Competitive Competitive NoncompetitiveNoncompetitive
AntagonistsAntagonists CompetitiveCompetitive NoncompetitiveNoncompetitive
PRESYNAPTIC MECHANISMSPRESYNAPTIC MECHANISMS
POSTSYNAPTIC MECHANISMSPOSTSYNAPTIC MECHANISMS
Psychoactive Drug ClassesPsychoactive Drug Classes CNS stimulantsCNS stimulants
amphetamine, cocaine, caffeine, nicotineamphetamine, cocaine, caffeine, nicotine CNS depressantsCNS depressants
alcohol, benzodiazepines, barbiturates, GHB alcohol, benzodiazepines, barbiturates, GHB HallucinogensHallucinogens
LSD, PCP, mescaline, MDMA(?)LSD, PCP, mescaline, MDMA(?) Narcotics (Opioids)Narcotics (Opioids)
morphine, methadonemorphine, methadone AntipsychoticsAntipsychotics
chlorpromazine, haloperidol, clozapine, chlorpromazine, haloperidol, clozapine, risperidonerisperidone
AntidepressantsAntidepressants SSRIs (e.g., Prozac, Paxil), MAOIs, tricyclicsSSRIs (e.g., Prozac, Paxil), MAOIs, tricyclics
Pharmacology of Psychoactive DrugsPharmacology of Psychoactive Drugs
Drugs with cholinergic actionsDrugs with cholinergic actions curare (nicotinic antagonist)curare (nicotinic antagonist) atropine (muscarinic antagonist)atropine (muscarinic antagonist) nicotine (nicotinic mixed agonist/antagonist)nicotine (nicotinic mixed agonist/antagonist)
Nonselective monoamine agonists Nonselective monoamine agonists reserpinereserpine MAO inhibitors (e.g., deprenyl)MAO inhibitors (e.g., deprenyl) tricyclic antidepressants (e.g., imipramine)tricyclic antidepressants (e.g., imipramine) CNS stimulants (e.g., cocaine, amphetamine)CNS stimulants (e.g., cocaine, amphetamine)
Pharmacology of Psychoactive DrugsPharmacology of Psychoactive Drugs
Other dopaminergic drugsOther dopaminergic drugs antipsychotics (haloperidol, chlorpromazine)antipsychotics (haloperidol, chlorpromazine) antiparkinson agents (L-DOPA, bromocriptine)antiparkinson agents (L-DOPA, bromocriptine)
Serotonergic drugsSerotonergic drugs SSRIs -- (Prozac, Paxil)SSRIs -- (Prozac, Paxil) LSDLSD
GABAergic drugsGABAergic drugs benzodiazepines (Valium, Xanax)benzodiazepines (Valium, Xanax) alcoholalcohol bicuculline (convulsant)bicuculline (convulsant)
Pharmacology of Psychoactive Pharmacology of Psychoactive DrugsDrugs