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Propranolol binds to β-adrenergic receptors with a KI of 8.9×10- 9M. What concentration of propranolol would be required to achieve a 50% reduction in the binding of the receptor agonist isoproterenol if the agonist concentration is 10 nM and its dissociation constant for the receptor is 4.8×10- 8M?

Short Answer

Expert verified

Concentration needed to achieve 50% reduction in binding is 1.1×10- 7M.

Step by step solution

01

Description

Beta-blockers are a class of medications that includes propranolol. It helps with anxiety, treats cardiac issues, and shields against migraines.Propranolol is a medication that can be used to treat high blood pressure if you have a heart condition.

02

Calculation of the concentration

The expression that connects the binding affinity of the competing ligand and the binding affinity of the bonded ligand is:

KI=[I]501 +[L]KL

KI of propranolol is8.9×10- 9M , the concentration of isoproterenol is[A] = 10 nM = 10- 8M,andKLof isoproterenol is 4.8×10- 8M.

03

Final result

So, the result is

I50=KI1 +[A]KL= 8.9×10- 91 +[10- 8]4.8×10- 8= 1.1×10- 7M

Therefore, the concentration needed to achieve 50% a reduction in binding is1.1×10- 7M.

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