Lecture 6 - Drug Targets

Question 1

Kd?

Answer 1

concentration of drug that ocupies 50% of receptor population

Question 2

Affinity vs biological response?

Answer 2

could take low level receptor occupancy to deliver maximal response (considerable amplification); downstream factors contributing to the final response

Question 3

Biological response figures?

Answer 3

EC50 and Emax

Question 4

Potency?

Answer 4

EC50 - the concentration of ligand to exert 50% maximal effect; more potent agonist has lower EC50

Question 5

Efficacy value and drug type?

Answer 5

positive Emax - agonist; negative - inverse agonist; zero - antagonist

Question 6

Definition of a partial agonist?

Answer 6

even at 100% affinity, cannot generate maximum response

Question 7

Tissue properties?

Answer 7

affect maximal response - an apparent partial agonist in one tissue can be a full agonist in another

Question 8

Antagonists on agonist response curve?

Answer 8

right shift = Rev.Com.Antag; Irreversible antagonist = drop in Emax (right shift in small doses due to non-requirement for 100% bonding)

Question 9

Irreversible AchE inhibitors?

Answer 9

highly toxic, very stable phospherous bonds which cannot be hydrolytically cleaved, build up of Ach in cleft, over excitation -> vomiting, shitting, sweating

Question 10

Diseases using AchE inhibitors?

Answer 10

Myasthenia gravis and Alzheimer’s