Receptor theory

4 important questions on Receptor theory

What is the pA2 value?

The affinity of a full competitive antagonist. It is the negative logarithm of the concentration of a competitive antagonist which requires a doubling of the agonist concentration to compensate for the antagonism.

What happens to the potency and efficacy of an agonist when you add a non-competitive antagonist?

The efficacy decreases, the potency doesn't change.

What is inverse agonism?

It is a substance that wants the receptor to be in the inactive state.
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What is the intrinsic activity of a full agonist, a partial agonist, an antagonist, an inverse agonist, and a partial inverse agonist?

Full agonist: α=1
Partial agonist: 0<α>1
Antagonist: α=0
Inverse agonist: α=-1
Partial inverse agonist: -1<α>0

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