HomeCoursesMEDSCI 204: Pharmacology and ToxicologyLecture 3 Lecture 3 1. What is the concentration response curve equivalent to binding Kd? EC50What is the concentration response curve equivalent to binding Kd?== EC50 2. What is another term for EC50? PotencyWhat is another term for EC50?== Potency 3. What is another term for EMax? EfficacyWhat is another term for EMax?== Efficacy 4. How to overcome an irreversible antagonist? Cell needs to make new receptorsHow to overcome an irreversible antagonist?== Cell needs to make new receptors 5. What is the primary binding site for the endogenous ligand called? Orthosteric binding siteWhat is the primary binding site for the endogenous ligand called?== Orthosteric binding site 6. What is an allosteric modulator? A ligand that binds to a site different than that of the orthosteric binding site and causes modulation to affinity, efficacy, or response (allosteric agonist)What is an allosteric modulator?== A ligand that binds to a site different than that of the orthosteric binding site and causes modulation to affinity, efficacy, or response (allosteric agonist) 7. What are the classes of allosteric modulators? Positive, negative, neutralWhat are the classes of allosteric modulators? ==Positive, negative, neutral 8. What is the ceiling effect of allosteric modulators? Extent of modulation is limited by cooperativity between orthosteric and allosteric ligand making overdose unlikelyWhat is the ceiling effect of allosteric modulators?== Extent of modulation is limited by cooperativity between orthosteric and allosteric ligand making overdose unlikely 9. How do allosteric modulators have increased selectivity compared to orthosteric ligands? Less of them - increased specificityHow do allosteric modulators have increased selectivity compared to orthosteric ligands?== Less of them - increased specificity 10. How is signalling of endogenous ligands maintained with allosteric modulation? Allosteric binding does not remove orthosteric binding...it mediates itHow is signalling of endogenous ligands maintained with allosteric modulation?== Allosteric binding does not remove orthosteric binding...it mediates it 11. How do drugs act on enzymes or transporters? They inhibit themHow do drugs act on enzymes or transporters?== They inhibit them 12. How do drugs inhibit enzymes? The occupy the active site of the enzymeHow do drugs inhibit enzymes?== The occupy the active site of the enzyme 13. What enzyme degrades ACh? AcetylcholineesteraseWhat enzyme degrades ACh?== Acetylcholineesterase 14. What are the classes of AChE? Irreversible, reversibleWhat are the classes of AChE? ==Irreversible, reversible 15. Where are irreversible AChEs used? Biological weapons eg. nerve gasWhere are irreversible AChEs used?== Biological weapons eg. nerve gas 16. How to overcome irreversible AChEs? Make more enzymeHow to overcome irreversible AChEs?== Make more enzyme 17. Where are reversible AChEs used? Alzheimer's, myasthenia gravis treatmentsWhere are reversible AChEs used?== Alzheimer's, myasthenia gravis treatments 18. What ways are neurotransmitters removed from a synapse? Transported, degradedWhat ways are neurotransmitters removed from a synapse?== Transported, degraded 19. How is seritonin removed from a synapse? Transported outHow is seritonin removed from a synapse? ==Transported out 20. What is the precurso to seritonin? TryptophanWhat is the precurso to seritonin?== Tryptophan 21. How is ACh removed from a synapse? DegradedHow is ACh removed from a synapse?== Degraded Loading...
