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quiz4a - 3 The IC 50 values for aspartate to bind to the...

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Quiz 4a - JAX True/False (2 pts. each) The following drugs all affect intracellular calcium levels: GABA, glutamate, aspartate, NMDA and kainate but MK801 has no effect (see Figure 1 next page). You have also measured and compared the efficacies and potencies of these drugs to displace the specific binding of 3 H-glutamate from homogenized brain samples (see Figure 2). Only 30% of the receptors occupied by 3 H-glutamate can bind kainate while only 70% of the receptors bind NMDA. Therefore, we conclude that there are two subtypes of glutamate receptor: 30% are the “K” subtype and 70% are the “N” subtype. Which of the following conclusions are true? If you don’t have any evidence to prove that the statement is true, then answer false. 1. Glutamate has a lower affinity for the "N" site compared to MK801’s affinity for the “N” site. 2. Glutamate binds to both “N” and “K” receptor subtypes but NMDA does not.
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Unformatted text preview: 3. The IC 50 values for aspartate to bind to the two subtypes are more similar than are the IC 50 values for glutamate to bind to the two subtypes. 4. Agonists for the "N" subtype of glutamate receptors increase intracellular calcium by positively activating that receptor subtype. 5. NMDA is a partial agonist at “N” receptors. 6. MK801 is an antagonist for the "N" subtype of glutamate receptors. 7. Kainate is an inverse agonist for the "N" subtype of glutamate receptors. Figure 1. Figure 2. 10 20 30 40 50 60 70 80 90 100 0.01 0.03 0.1 0.3 1 3 10 30 100 300 1000 3000 Competing Drug concentration (nM) % Specific 3H-glutamate Binding Kainate MK801 Glutamate GABA NMDA Aspartate 20 40 60 80 0.01 0.03 0.1 0.3 1 3 10 30 100 300 1000 3000 Drug Concentration (nM) Intracellular Calcium levels (uM) NMDA Asp. Glu. GABA MK801 Kainate...
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  • Spring '07
  • veige/martin
  • Receptor antagonist, NMDA receptor, Inverse agonist, glutamate receptors, intracellular calcium levels

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