26. Carbonic anhydrase is strongly inhibited by the drug acetazolamide, which is used as a diuretic and to lower excessively high pressure in the eye in glaucoma. Carbonic anhydrase plays an important role in these and other secretory processes because it participates in regulating the pH and bicarbonate content of several body fluids. The experimental curve of initial reaction velocity (as percentage of Vmax) versus (S] for the carbonic anhydrase reaction is illustrated below. When the experiment is repeated in the presence of acetazolamide, the lower curve is obtained. 100 No inhibiter 50 Acetazolamide 0.2 0.4 0.6 0.8 a. What happens to Vmas in the presence of the enzyme (E) and enzyme plus inhibitor (EI)? IS] (mM) b. What does the graph tell you about the ratios of Vmaxt/max(t)? c. What does the graph tell you about the concentration of (S] as the rate approaches Vmax with and without inhibitor? d. From an inspection of the curves and your knowledge of the kinetic properties of competitive, non- competitive and mixed non-competitive enzyme inhibitors what is the nature of the inhibition of acetazolamide? Explain. APSIA

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Chapter15: Fluid And Acid-base Balance
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26. Carbonic anhydrase is strongly inhibited by the drug
acetazolamide, which is used as a diuretic and to lower
excessively high pressure in the eye in glaucoma.
Carbonic anhydrase plays an important role in these and
other secretory processes because it participates in
regulating the pH and bicarbonate content of several
body fluids. The experimental curve of initial reaction
velocity (as percentage of Vmax) versus (S] for the
carbonic anhydrase reaction is illustrated below. When
the experiment is repeated in the presence of
acetazolamide, the lower curve is obtained.
100
No inhibitor
* 50-
Acetazolamide
0.2
0.4
0.6
0.8
SJ (mt)
a. What happens to Vmax in the presence of the enzyme
(E) and enzyme plus inhibitor (EI)?
b. What does the graph tell you about the ratios of Vmax(t/Vmax(tn?
c. What does the graph tell you about the concentration of [S] as the rate approaches Vmax with and
without inhibitor?
d. From an inspection of the curves and your knowledge of the kinetic properties of competitive, non-
competitive and mixed non-competitive enzyme inhibitors what is the nature of the inhibition of
acetazolamide? Explain.
V(% of Vm
Transcribed Image Text:26. Carbonic anhydrase is strongly inhibited by the drug acetazolamide, which is used as a diuretic and to lower excessively high pressure in the eye in glaucoma. Carbonic anhydrase plays an important role in these and other secretory processes because it participates in regulating the pH and bicarbonate content of several body fluids. The experimental curve of initial reaction velocity (as percentage of Vmax) versus (S] for the carbonic anhydrase reaction is illustrated below. When the experiment is repeated in the presence of acetazolamide, the lower curve is obtained. 100 No inhibitor * 50- Acetazolamide 0.2 0.4 0.6 0.8 SJ (mt) a. What happens to Vmax in the presence of the enzyme (E) and enzyme plus inhibitor (EI)? b. What does the graph tell you about the ratios of Vmax(t/Vmax(tn? c. What does the graph tell you about the concentration of [S] as the rate approaches Vmax with and without inhibitor? d. From an inspection of the curves and your knowledge of the kinetic properties of competitive, non- competitive and mixed non-competitive enzyme inhibitors what is the nature of the inhibition of acetazolamide? Explain. V(% of Vm
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