Enalapril is an anti-hypertension "prodrug" (i.e., a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. ▾ Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? Submit Part B O Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation. O Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation. Request Answer μA K₁ = Value 7 Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin I. ACE has a KM = 52 M for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat? Express your answer to two significant figures and include the appropriate units. PX? EtOOC Units -NH O B CH₂ N HOOC Enalapril
Enalapril is an anti-hypertension "prodrug" (i.e., a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. ▾ Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? Submit Part B O Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation. O Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation. Request Answer μA K₁ = Value 7 Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin I. ACE has a KM = 52 M for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat? Express your answer to two significant figures and include the appropriate units. PX? EtOOC Units -NH O B CH₂ N HOOC Enalapril
Chapter10: Reconstitution Of Powdered Drugs
Section: Chapter Questions
Problem 3.4P
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Question
82.23
Transcribed Image Text:Enalapril is an anti-hypertension "prodrug" (i.e., a drug
precursor) that is inactive until the ethyl ester (arrow in
figure) is hydrolyzed by esterases present in blood plasma.
The active drug is the dicarboxylic acid ("enalaprilat") that
results from this hydrolysis reaction.
Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but
enalaprilat does not?
Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation.
Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation.
Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation.
Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation.
Submit
Part B
K₁ =
Request Answer
Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide
angiotensin I. ACE has a KM = 52 μM for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is
present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat?
Express your answer to two significant figures and include the appropriate units.
Submit
HA
Value
EtOOC
-NH
O
33
CH3
HOOC
Enalapril
Request Answer
Units
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