Enalapril is an anti-hypertension \"prodrug\" (i. e., a drug precursor) that is

Question

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 this hydrolysis reaction. Part A Enalapritat is a competitive inhibitor of angiotensin-converting enzyme (ACE), which cleaves the blood pressure regulating peptide angiotensin 1. ACE has a K_M = 52 mu M for anglotensin 1, which is present in plasma at a concentration of 75 mu M. When enalaprilat is present at 2.4 nM, the activity of ACE in plasma is 10 % of its uninhibited activity. What is the value of K_1 for enalaprilat?

Explanation / Answer

simple:

for K1 we need

alpha = sqrt(K1/C)

then

10% --< 10/100 = 0.10

and we have

C = 2.4 nM = 2.4*10^-9 M

so

solve for K1

K1 = a^2 * C

K1 = (0.1^2)(2.4*10^-9) = 2.4*10^-11

K1 = 2.4*10^-11 M

Related Questions

Navigate

• Browse (All)
• Browse E
• Subjects

---

---

Integrity-first tutoring: explanations and feedback only — we do not complete graded work. Learn more.