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Study of the effects of drugs on the nervous system and behavior |
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The changes we can observe in an organism's physiological process ands behavior |
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Location at which the drug molecules interact with molecules on or in the cell thereby affecting the processes in these cells |
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-Ligands made in the body - Neurotransmitter and neuromodulators |
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-Ligands not made in the body -Drugs and biological toxins |
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Process by which drugs are absorbed, distributed within the body, then metabolized and excreted |
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Factors that affect rate of drug into brain |
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-Lipid solubility - Ionization -Size |
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Highly lipid soluble molecules can pass lipid barriers quickly |
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Uncharged molecules pass through membranes quickly |
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Small molecules pass through membranes more quickly than larger ones |
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-Deactivation of drugs by enzymes -Liver plays a large role -Enzymes metabolize drugs into another substance that is biologically active |
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-Primarily in urine -Kidney is responsible for pushing out drug |
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Dose Response curve (D-R curve) |
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A graph of the magnitude of an effect of a drug as a function of the amount of drug administered |
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The readiness with which 2 molecules join together |
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The ratio between the doses that produce the desired effect in 50% of the animals vs the dose that produces toxic effects in 50% of the animals -High: safe drug -Low: not a very safe drug |
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-A ligand that binds to produce a full effect -Facilitates the effect of a neurotransmitter |
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- a ligand that binds and produces no effect -Opposes the effects of a neurotransmitter |
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-ligand that binds and produces the full effect |
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Ligand the binds and produces a partial effect |
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Ligand that binds to a different site on the receptor than the neurotransmitter and facilitates the actions of the neurotransmitter once it has bound |
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Ligand that binds to a different site on the receptor but prevents the neurotransmitter from having an effect onice it binds |
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Drug effect on production of neurotransmitters |
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-Synthesis is controlled by enzymes -Drugs can affect the enzymes thereby affecting synthesis |
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Drug effect on storage & release of neurotransmitters |
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-Drugs can affect the transport molecules -Drugs can interfere with vesicles and release |
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Drug effect on reuptake and destruction of neurotransmitters |
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-Drugs can interfere with theses processes. |
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-An ion channel opens in response to ligand binding -Can result in an EPSP/IPSP depending on ion channel |
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-An intracellular cascade of events begins in response to agonist binding - Can result in an EPSP/IPSP or a change in the intracellular environment. |
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-Activation results in an IPSP or EPSP depending on type of receptor |
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-Receptors located on the presynaptic neuron that are sensitive to the neurotransmitter that it releases -Mostly Inhibitory/ negative feedback |
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Receptors located on the presynaptic button that are sensitive to a neurotransmotter that is different than the one released by the neuron |
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-A chemical released by a presynaptic element upon stimulation that activates postsynaptic receptors -Usually full agonists at primary receptor site. -Causes EPSP or IPSP in postsynaptic membrane -Act as neuromodulators |
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-Primary neurotransmitter secreted by efferent neurons of the CNS -1st neurotransmitter discovered -Widely throughout the brain -Usually is excitatory |
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-Ionotropic receptor -Primarily gates Na+ -EPSP -Fast -2 ACh molecules need to bind to active the receptor |
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-G-protein coupled receptors -5 subtypes -Different subtypes are coupled to different G-proteins -Slower |
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-ACh agonist -Triggers release of ACh |
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-ACh antagonist -Prevents release of ACh by the terminal buttons |
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-All have one amine group -Similar molecular structure -Drugs tend to affect activity in all of them -Includes Epinephrine (EPI/andrenaline), Norepinephrine (NE), Dopamine (DA) |
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-Involved in Movement, attention, learning, & reward and motivation -3 major projection systems in the brain -5 receptor subtypes (D1-D5) -Can produce IPSP/EPSP |
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-Dopaminergic cell bodies in the substantia nigra (SN) that project and have terminal buttons in the neostriatum -Involved in movement |
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-Dopaminergic cell bodies located in the ventral tegmental area (VTA) that project and have terminal buttons in the nucleus accumbens (NAC) and amygdala -Involved in reward and motivation |
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-Dopaminergic cell bodies located in the VTA that project and have terminal buttons in the prefrontal cortex -Involved in short-term memory, planning and problem solving |
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-precursor is modified in each step by an enzyme -precursor for catechomines is tyrosine -tyrosine is converted to L-DOPA by the enzyme tyrosine |
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Reuptake from synaptic cleft into presynaptic neurons |
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Enzyme that breaks down monoamines intrauneronally |
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Catechol-O-methyltransferase (COMT) |
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-Enzyme that breaks down catecholamines extraneuronally |
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-Indirect DA agonist -treatment fro Parkinson's disease |
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-DA receptor antagonist -treatment for schizophrenia |
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-Found in neurons in the ANS -important neurotransmitter in the brain -involved in arousal -release is at axonal varicosities |
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-Hormone produce by adrenals |
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-In every psychological function -Involed in temperature regulation, sleep, learning memory, sexual functions, hormonal secretions, etc |
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-Contains serotonergic cell bodies that project up to the cerebral cortex and basal ganglia |
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-Has serotonergic cell bodies that project up to the cerebral cortex and hippocampus. |
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-5-Ht agonist -blocks the reuptake of 5-HT -treatment for depression,anxiety disorders, and OCD |
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Lysergic acid diethylamide (LSD) |
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-5-HT receptor agonist -produces halluncinations |
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-8 suspected amino acid transmitters -An excitatory amino acid transmitter -Major excitatory neurotansmission in the brain -Involved in working memory, perception and voluntary muscle control |
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Gamma-aminobutyric acid (GABA) |
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-Inhibitory amino acid neurotransmitter -Primary inhibitory transmission in the brain -Keeps excitatory Glu transmission in check -40% of all brain synapses show this activity |
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-Too much glu= epilepsy and exitotoxicity -too much GABA- no LTP |
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-GABA allosteric agonists |
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