NEURONS & NEURAL TRANSMISSION NEUROCHEMICAL MECHANISMS OF DRUG ACTION

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