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NEURONS & NEURAL TRANSMISSION NEUROCHEMICAL MECHANISMS OF DRUG ACTION

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

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NEURONS & NEURAL TRANSMISSION NEUROCHEMICAL MECHANISMS OF DRUG ACTION

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  1. NEURONS&NEURAL TRANSMISSIONNEUROCHEMICAL MECHANISMS OF DRUG ACTION

  2. 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

  3. CNS ORGANIZATION

  4. Autonomic Nervous System

  5. NEURONS

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

  7. MEMBRANE POTENTIAL

  8. ACTION POTENTIAL

  9. ACTION POTENTIAL

  10. CONDUCTION OF A.P.

  11. NEURONAL COMMUNICATION • POSTSYNAPTIC POTENTIALS • Excitatory PSP • Inhibitory PSP

  12. NEUROCHEMICAL SYNAPSE • Presynaptic Membrane • Postsynaptic Membrane • Synaptic Vesicles • Synaptic Cleft • Receptor Sites

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

  14. SYNTHESIS

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

  16. 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

  17. NEUROCHEMICAL PATHWAYS

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

  19. RECEPTOR ACTIVATION

  20. DRUG ACTIONS ON RECEPTOR ACTIVATION • Agonists • Competitive • Noncompetitive • Antagonists • Competitive • Noncompetitive

  21. PRESYNAPTIC MECHANISMS

  22. POSTSYNAPTIC MECHANISMS

  23. 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

  24. 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)

  25. 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)

  26. Pharmacology of Psychoactive Drugs

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