Antagonism - stopping things from happening

Question 1

What are the 3 categories of antagonists?

Answer 1

competitive antagonists, non competitive antagonists at a receptor - allosteric inhibitors, non competitive antagonists not at receptor - functional antagonists or pathway inhibitors

Question 2

What stage of drug pathways do competitive antagonists stop?

Answer 2

binding

Question 3

What stage of drug pathways do pathway inhibitors stop?

Answer 3

activation

Question 4

What stage of drug pathways do functional antagonists stop?

Answer 4

transduction

Question 5

How do allosteric inhibitors change drug action?

Answer 5

Either by changing the affinity of the receptor for the endogenous ligand, by modulating endogenous ligand efficacy or by modulating receptor activation level

Question 6

Why is allosteric modulation important?

Answer 6

Because allosteric binding sites are specific to each receptor subtype and so therefore the agent can be selective, also because physiological modulation is still possible on top of allosteric modulation

Question 7

What is surmountability?

Answer 7

The ability to be overcome

Question 8

Are competitive reversible antagonists surmountable?

Answer 8

in the lab yes but not necessarily in vivo

Question 9

Are non competitive antagonists surmountable?

Answer 9

No