24 Questions
What is the structural feature that gives pentameric superfamily receptors their name?
Cys-cys looping
Which drug acts as a competitive antagonist of most GABAAR's?
Bicuculline
Which drug enhances the actions of GABA and known to be more selective?
Benzodiazepines
Which drug can act alone or enhance the actions of GABA and is less selective, making it more dangerous?
Barbiturates
Which subunits are selective for benzodiazepines in GABAAR receptors?
α1-3,5 and γ
Which drug acts on all GABAA receptors?
Barbiturates
What effect is mediated by the α2 subunit of GABAAR receptors when benzodiazepines are present?
Anxiolysis
How can the effects of benzodiazepines be eliminated?
Replacing the Histidine residue with an Arginine residue
Which drug binds to the TM domain of GABA receptors and enhances GABA?
Ethanol
Which drug directly stimulates GABA receptors at high concentrations?
General anaesthetics
Which drug alters the pore conformation of M2 in GABA receptors?
Propofol
Which drug is an allosteric enhancer of GlyRs?
Ivermectin and Cannabinoids
Which drug is an antagonist of 5HT3R?
Ondansetron
Which drug is used to treat IBS?
Alosetron
Which type of receptors are voltage dependent and can be blocked by Mg2+?
NMDA-R
What is the role of glycine in NMDA-R activation?
It acts as a co-agonist
What is the structure of excitatory GluR's?
Tetrameric
Which molecules act as agonists on GluR's?
NMDA, kainate, AMPA, glutamate
Which type of receptors have increased selectivity for their respective receptors due to increased rigidity?
AMPA-R
Which binding site on AMPA-R's is responsible for uncompetitive antagonists?
Ion channel pore
Which part of GluR's structure contains the selectivity filter on the pore?
TMD (transmembrane domain)
What confers selectivity in the M2 helices of the structure?
Charged residues
What happens to the α-helices when the pore is closed?
They bend inward
What occurs to the helices when the pore opens?
They tilt and rotate
Test your knowledge on pentameric superfamily receptors and excitatory ionotropic glutamate receptors with this quiz. Identify various receptors and their functions, including nAChR, 5-HT3 R, GlyR, GABAAR, AMPA, NMDA, Kainate, and ATP receptors. Explore the effects of endogenous ligands on ion channels.
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