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25 Cards in this Set
- Front
- Back
Which of the 5-HT families is ionotrophic?
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5-HT3
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Which family of 5-HT receptors is associated with sleep, thermo-regulation, learning, appetite control, sensory reception and hallucinogens?
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5-HT2
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Which family of 5-HT receptors can be found on a presynaptic neuron?
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5-HT1 (specifically family D)
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Are most 5-HT families ionotrophic or G-protein coupled?
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G-protein coupled
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Is Tryptophan hydroxylase involved in biosynthesis or degradation of serotonin?
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biosynthesis
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Is aromatic amino acid decarboxylase involved in either biosynthesis or degradation of serotonin?
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biosynthesis
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Is Aldehyde/Keto reductase involved in either biosynthesis or degradation of serotonin?
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degradation
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Is aldehyde reductase involved in either biosynthesis or degradation or serotonin?
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degradation
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What is the primary function of 5-HT2A antagonists?
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Atypical antipsychotics
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What effect do many 5-HT2A agonists have?
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They enhance "tripping rate"
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What class of 5-HT drugs do cozapine and risperidone belong to?
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5-HT2A antagonists
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What was the popular drug Fen-Phen used for? What two types of drug was it made up of?
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Weight loss; 5-HT2c agonist (fenfluramine) + norepinephrine releasing agent (phenteramine)
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What do 5-HT3 receptors modulate the release of?
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Other neurotransmitters like dopamine, Ach, and serotonin
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What class of antidepressants is no longer used due to severe side effects?
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MAO (monoamine oxidase) inhibitors
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What are four key structural features of MAO irreversible inhibitors?
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Hydrazide, hydrazine, terminal alkyne and benzylic cyclopropane
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Which isoform of MAO is most closely associated with depression?
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Isoform B
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True or False: All MAO inhibitors bind covalently and thus irreversibly.
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False.
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What are 5-HT3 antagonists used to treat?
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Nausea.
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What is the mechanism of fluoxetine and paroxetine?
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Serotonin re-uptake inhibitors (SSRI)
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Which enzyme would convert imipramine to desipramine, and how does it accomplish this?
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CYP2D6; dealkylation (removes a methyl group)
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What is a proposed mechanism for imipramine to inhibit CYP2D6?
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The formaldehyde lost may react with the CYP2D6 enzyme, rendering it inactive.
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What does SNRI stand for?
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serotonin norepinephrine reuptake inhibitor
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What is an advantage of using SSRIs instead of TCAs?
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Decreased side effects such as dry mouth, dizziness and cardio-toxicity.
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Which group of antidepressants work by attempting to restore both NE and 5-HT without side effects?
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SNRIs
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What is the goal associated with the Biogenic Amine Hypothesis of Depression?
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The goal is develop drugs that increase overall adrenergic and/or serotonergic levels in the CNS
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