NEURONS & NEURAL TRANSMISSION NEUROCHEMICAL MECHANISMS OF DRUG ACTION

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Presentation transcript:

NEURONS & NEURAL TRANSMISSION NEUROCHEMICAL MECHANISMS OF DRUG ACTION

Nervous System Divisions CNS (central nervous system) Brain, Spinal Cord 12 pairs of cranial nerves (originate from cranium) PNS (peripheral nervous system) Somatic nervous system 31 pairs of spinal nerves Autonomic nervous system

CNS ORGANIZATION

Autonomic Nervous System

NEURONS

NEURON MEMBRANE Membrane Structure Semipermeable lipid bilayer Proteins Ion channels Transport pumps Receptors

MEMBRANE POTENTIAL

ACTION POTENTIAL

ACTION POTENTIAL

CONDUCTION OF A.P.

NEURONAL COMMUNICATION POSTSYNAPTIC POTENTIALS Excitatory PSP Inhibitory PSP

NEUROCHEMICAL SYNAPSE Presynaptic Membrane Postsynaptic Membrane Synaptic Vesicles Synaptic Cleft Receptor Sites

SYNAPTIC TRANSMISSION Synthesis Storage Neurotransmitter Release Receptor Activation Neurotransmitter Deactivation Enzymatic Deactivation (Metabolism) Reuptake

SYNTHESIS

NEUROTRANSMITTER FAMILIES Acetylcholine Monoamines Norepinephrine Dopamine Serotonin Amino Acid Transmitters Glutamate GABA Histamine Glycine Neuropeptides Enkephalins Endorphins

Receptor Subtypes for Neurotransmitters 4/25/2017 Receptor Subtypes for Neurotransmitters Acetylcholine: nicotinic, muscarinic Dopamine: D1, D2, D3, D4, D5 Norepinephrine: alpha1, alpha2, beta1, beta2 Serotonin: 5-HT1a,1b,1c,1d; 5-HT2a,2b,2c;; 5-HT3… GABA: GABAA, GABAB Glutamate: NMDA, AMPA, mGluR Endorphins: mu, kappa, delta

NEUROCHEMICAL PATHWAYS

RECEPTOR ACTIVATION Ligand-gated ion channels Ionotropic Receptors Metabotropic Receptors G proteins Second Messengers

RECEPTOR ACTIVATION

DRUG ACTIONS ON RECEPTOR ACTIVATION Agonists Competitive Noncompetitive Antagonists

PRESYNAPTIC MECHANISMS

POSTSYNAPTIC MECHANISMS

Psychoactive Drug Classes CNS stimulants amphetamine, cocaine, caffeine, nicotine CNS depressants alcohol, benzodiazepines, barbiturates, GHB Hallucinogens LSD, PCP, mescaline, MDMA(?) Narcotics (Opioids) morphine, methadone Antipsychotics chlorpromazine, haloperidol, clozapine, risperidone Antidepressants SSRIs (e.g., Prozac, Paxil), MAOIs, tricyclics

Pharmacology of Psychoactive Drugs Drugs with cholinergic actions curare (nicotinic antagonist) atropine (muscarinic antagonist) nicotine (nicotinic mixed agonist/antagonist) Nonselective monoamine agonists reserpine MAO inhibitors (e.g., deprenyl) tricyclic antidepressants (e.g., imipramine) CNS stimulants (e.g., cocaine, amphetamine)

Pharmacology of Psychoactive Drugs Other dopaminergic drugs antipsychotics (haloperidol, chlorpromazine) antiparkinson agents (L-DOPA, bromocriptine) Serotonergic drugs SSRIs -- (Prozac, Paxil) LSD GABAergic drugs benzodiazepines (Valium, Xanax) alcohol bicuculline (convulsant)

Pharmacology of Psychoactive Drugs