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PSYC 214: Ch. 4
Neuropharmacology
| Question | Answer |
|---|---|
| How can an agonist exogenous ligand increase excitatory effect? | by opening up more receptors for the excitatory neurotransmitter it's mimicking |
| How can an antagonist exogenous ligand increase excitatory effect? | by blocking more receptors of the inhibitory neurotransmitter |
| How can an antagonist exogenous lgand increase inhibitory effect? | by blocking more receptors of the excitatory neurotransmitter |
| How can an exogenous agonist increase inhibitory effect? | by opening up more receptors for the inhibitory neurotransmitter it's mimicking |
| competitive ligand | binds to same receptor site as the endogenous neurotransmitter; can be agaonist or antagonist |
| noncompetitive ligand | binds to another modulatory site on the same receptor as the endogenous neurotransmitter; can be agonist or antagonist |
| binding affinity | the degree of chemical attraction between a ligand & a receptor |
| high (binding) affinity | very selectively binds to a very specific receptor low doses necessary for effect binds for a longer time than most other neurotransmitters (in terms of milliseconds) |
| low (binding) affinity | fewer molecules bind to receptors higher doses necessary for effect binds for shorter time may be less selective in that it binds to sites of neurotransmitters doing a specific function, but it's not selective to a specific neurotransmitter |
| efficacy | propensity for a ligand to activate the receptor aka: after it binds to a site, what will it do & how effective will it be? |
| Quaternary amines: | Acetylcholine (ACh) |
| Monoamines: (Catecholamines & Indoleamines) | Catecholamines: Dopamine (DA) & Norepinephrine (NE) Indoleamines: Serotonin (5-HT) |
| Neuropeptides: | peptide hormones, Oxytocin (OT), & Vasopressin (AVP) |
| Amino Acids: | GABA & Gluatamate |
| Agonists have ----- efficacy, Antagonists have ----- efficacy | high low; antagonists also might have high affinity |
| dose-response curve | relation between drug & observed effect |
| ED50- LD50- | ED50- effective dosage at which 50% of subjects experience desired effect LD50- lethal dosage for 505 of subjects |
| How do neurons become tolerant? | number of receptors change, NOT number of neurotransmitters |
| tolerance | where drug becomes less effective |
| 2 types of tolerance: | metabolic tolerance functional tolerance |
| metabolic tolerance | organs metabolize the drug; body adapts to it |
| functional tolerance | tolerance occurs at the target tissue; brain adapts to it |
| tolerance at the receptor: repeated exposure to agonist | neurons down-regulate receptor |
| tolerance at the receptor: repeated exposure to antagonist | neurons up-regulate receptor |
| neurotransmitters are classified based on their ------ components | chemical |
| peptide hormones | made primarily in the hypothalamus receptors throughout limbic system |
| Oxytocin (OT) & Vasopressin (AVP) | peptides modulate social behaviors receptor concentration & receptor location determines how they affect social behaviors |
| it's not so much the amount of a receptor there is that's important in affecting social behaviors, its the receptor --------- & --------- | location & concentration |
| Acetylcholine (ACh) has 2 receptor types: | Nicotinic Muscarinic |
| ACh Nicotinic receptor | ionotropic excitatory |
| localization & function of ACh Nicotinic receptor | neuromuscular synapses midbrain - movement midbrain - reward - ventral tegmented area |
| curare | antagonist drug/poison nicotinic ACh receptor used by muscles to cause paralysis |
| ACh Muscarinic receptor | metabotropic G protein coupled excitatory or inhibitory |
| localization & function of ACh Muscarinic receptor | cells project to hippocampus learning & memory |
| localization of dopaminergic receptors | dopaminergic neurons are found in mesostriatal pathway & mesolimbocortical pathway |
| mesostriatal pathway/system | movement & motor control substantia nigra (midbrain)- contains one of the largest clusters of dopaminergic cells in the brain basal ganglia- substantia nigra, striatum (caudate + putamen, globus pallidus |
| mesolimbocortical pathway/system | midbrain to limbic system motivated behaviors - reward components DA - release following positive stimuli - graded response ventral tegmental area - nucleus accumbens overactivity is a sympton of schizophrenia |
| Parkinson's/Parkinson's-like symptoms | dr. oliver sacks L-dopa = exogenous agonist tolerance neurons down-regulate the receptor |
| Dopamine receptor subtypes | D1, D2, D3, D4, D5 effectiveness of antipsychotics depends on affinity to bind to D2 receptor antipsychotics bind the receptor as antagonist (selective antagonist) neuroleptics - haloperidol |
| cholinergic pathways | produces ACh |
| the 2 main clusters of neurons in the brain stem releasing Norepinephrine (NE) are the --- ----- in the pons & the ------- ------- system of the midbrain | locus coeruleus lateral tegmental |
| noradrenergic | NE-producing cells, because norepinephrine is also known as noradrenaline |
| excitotoxicity | a phenomenon in which neural injury provokes an excessive release of glutamate that produces prolonged depolarization of postsynaptic cells |
| the most common transmitters in the brain are- | amino acids |
| opiod peptides | peptides that can't mimic opiate drugs, such as morphine |
| selective serotonin reuptake inhibitor (SSRI) name 3 popular examples: | SSRI- a drug that blocks the reuptake of transmitter at serotinergic synapses examples: Prozac, Zoloft, Citalpram |
| monoamine oxidase (MAO) | MAO- an enzyme that breaks down & thereby inactivates monoamine transmitters |
| Serotonin (5-HT) has -- receptor types. It is produced in the ----------- & the ---- ------ (in midbrain & brainstem) | 15. mesencephalic & ralphe nuclei |
| serotonin has been implicated in the control of- | sleep states, mood, sexual behavior, anxiety, etc. antidepressants increase serotinergic activity |
| MAOI | monoamine oxidase inhibitors |
| Serotonin is involved with the processing of the ---------- system & of ----------- | sensory perception |
| Tricyclics Name one historical type of Tricyclic | block reuptake of serotonin (& norepinephrine) Tofranil |
| things that affect serotoin receptors: | MAOI, Tricyclics, SSRI, Hallucinogens |
| mesencephalic serotinergic cells project to -----, ---- --- & ------ | thalamus, basal ganglia, & cortex |
| major excitatory amino acid- major inhibitory amino acid- | gluatamate GABA |
| amino acid Gluatamate | always excitatory receptors- ionotropic: AMPA, Kainate, NMDA (crucial for learning & memory to occur in hippocampus) associated with excitotoxicity receptors- metabotropic: mGluR's (act more slowly because they work through 2nd messengers |
| amino acid GABA | always inhibitory 3 main receptors: GABA A- ionotropic GABA B- metabotropic GABA C- ionotropic combination of protein subunits = hundreds of different GABA receptors blocking GABA receptors = seizures, tremors, uncontrolled movements, shakes |
| metabotropic receptor | receptor & ion channel are not the same component 2-step process results in greater versatility in how the neuron can respond process for G protein coupled receptors slower can be excitatory or inhibitory |
| ionotropic receptor | ion channel & receptor are the same unit faster can be excitatoyr or inhibitory ligand-gated ion channel |
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