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53 Cards in this Set
- Front
- Back
Neurotransmission in the CNS occurs mostly with these three amino acids:
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1. γ-aminobutyric acid (GABA), 2. glutamic acid (glutamate [Glu]) and
3. glycine |
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What % of all neurons in the CNS use GABA as a neurotransmitter substance?
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40%
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Less than 10% of neurons use one of the other monoamine types which are:
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NE, serotonin, and acetylcholine
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Amino acid neurotransmitters are subcategorized into
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excitatory and inhibitory
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Four excitatory amino acid neurotransmitters
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1. glutamate (Glu)
2. aspartate (Asp) 3. cysteine 4. homocysteine |
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Four inhibitory amino acid neurotransmitters
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1. GABA
2. glycine (Gly) 3. taurine 4. β-Alanine |
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When neuronal cells are at rest, are the ion channels opened or closed?
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closed
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When a neuron is depolarized, what ion types are entering the cell through channels?
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Na+ and Ca2+
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When the neuron is _________, the membrane potential is more positive and in turn more likely to exhibit an action potential causing an electrical current to flow to other points in the membrane
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depolarized
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When a neuron is __________, K+ moves out of the cell into extracellular space or Cl- moves into the cell
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hyperpolarized
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Ion fluxes of K+ or Cl- results in this, which decreases the likelihood that a neuronal cell will fire
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hyperpolarization
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Excitatory membrane potential is also known as
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depolarization
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Inhibitory membrane potential is also known as
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hyperpolarization
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The two nonresting states of neuronal cells:
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excitatory and inhibitory
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During this nonresting state, Na+ or Ca2+ ions move into the cell, making the membrane potential grow until action potential is reached
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excitatory
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During this nonresting state, Cl- moves into the cell or K+ moves out of the cell, causing the neuron to return to resting state
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inhibitory
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The major EEA (excitatory amino acid) neurotransmitter in the CNS is ________, which is found in all cells in the CNS
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L-glutamate
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This EEA is a precursor in the biosynthesis of inhibitory neurotransmitter GABA
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glutamate
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The receptors for glutamate and other EEAs are categorized into two major groups
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ionotropic and metabotropic
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These EEA receptors are associated with ligand-gated ion channels
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ionotropic
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The three ionotropic receptor types are classified based on their ________ _________ for the EAA ligands
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selective affinity
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1. N-methyl-D-aspartate (NMDA)
2. α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) and 3. kainite |
ionotropic receptor types
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This is a homologue of the neurotoxin ibotenic acid found in Amanita mushrooms
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AMPA, ionotropic receptor
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This is a neurotoxin isolated from red algae
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Kainate, ionotropic receptor
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This EAA ionotropic receptor subtype increases Na+ and Ca2+ INFLUX and increases K+ EFFLUX
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AMPA
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This EAA ionotropic receptor subtype increases Na+ INFLUX and increases K+ EFFLUX
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kainate
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This EAA ionotropic receptor subtype increases Ca2+ INfLUX and increases K+ EFFLUX and glycine
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NMDA
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Is glutamate an agonist or antagonist for each of the EAA ionotropic receptor subtypes?
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Agonist
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Activation of EAA metabotropic receptors results in alterations in these processes within the cell
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metabolic processes
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All of these EAA receptors are activated by glutamate and ibotenate
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metabotropic receptors
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Are any of the metabotropic receptors activated by NMDA, AMPA or kainate?
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None of them are activated
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The major inhibitory amino acid (IAA) neurotransmitter in the mammalian CNS is
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γ-Aminobutyric Acid (GABA)
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How many different families of GABA receptors are identified
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three, A,B,C
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This IAA receptor was the first to be identified and is a ligand-gated ion channel
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GABA
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What major class of compound modulates GABAa receptor function?
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benzodiazepines (e.g. diazepam)
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The second most common inhibitory amino acid neurotransmitter in the CNS
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glycine
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Agents that act as agonists at this IAA receptor may be anticonvulsants, muscle relaxants, sedatives and general anesthetics
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glycine receptor
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The best described ANTAGONIST of the inhibitory glycine receptor is this convulsant
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styrchnine
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The inhibitory glycine receptor is sometimes referred to as this in order to distinguish it from a glycine site on the NMDA receptor
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strychnine-sensitive glycine receptor
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This agent has also been shown to antagonize the activity of glycine at its receptor (NOT strychnine)
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anandamide
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These reversibly block the nerve conductances that transmit the feeling of pain to the brain
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local anesthetics
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Do general and local anesthetic drugs block nerve conductance in both sensory and motor neurons or just one of them?
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both sensory and motor
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Do general anesthetics cause loss of consciousness or impairment of vital functions?
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NO
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Are coca leaves (cocaine) known to have local or general anesthetic properties?
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local
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Benzoylatropine is the same chemical structure as cocaine but is missing which functional group?
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ester functional group
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Benzoylatropine led to the discovery of which other drug
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procaine
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Is cocaine a vasodilator or vasoconstrictor?
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vasoconstrictor
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All procaine-derived local anesthetics are associated with what property
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vasodilation
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In order to decrease the rate of removal of procaine-derived local anesthetics from the site of administration, a vasoconstrictor like this is commonly used
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epinephrine
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This local anesthetic is most widely used
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lidocaine
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These two cyclic nucleotides play critical roles in mediating cellular signals in response to hormones, neurotransmitters, chemokines and cytokines
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cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP)
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These hydrolyze the cyclic nucleotides to their inactive linear forms (5'-AMP and 5'-GMP)
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phosphodiesterases (PDEs)
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Vardenafil (Levitra), Sildenafil (Viagra) and Tadalafil (Cialis) are all developed for the Tx of male erectile dysfunction
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selective PDE5 inhibitors
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