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25 Cards in this Set

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