The structure Endothelin-1 contains two ____ bonds between two____ amino acids.
A. Covalent, Threonine
B. Ionic, Cysteine
C. Disulfide, Cysteine
D. Hydrogen, Cysteine
ET-1 concentrations are ____ in patients presenting with PAH, leading to increased _____
A. Increased, Vasoconstriction
B. Increased, Vasodilation
C. Decreased, Vasoconstriction
D. Decreased, Vasodilation
In the structure of Bosentan (Tracleer) the following functional group undergoes _____ through the enzyme _____
A. Oxidation, 2C9
B. Hydrolysis, 2C9
C. O-demethylation, 2C9
D. Methylation, 2C9
In the structure Bosentan (Tracleer) the circiled group undergoes ____ in order to produce the ___ metabolite
A. Hydroxylation, Inactive
B. Hydroxylation, Active
C, Reduction, Inactive
D. Reduction, Active
Which of the following statments is true regarding Bosentan?
A. Hydroxylation at the red portion will create a minor inactive metabolite
B. O-demethylation at the blue portion will create a minor inactive metabolite
C. Hydroxylation at the red portion will create a major active metabolite
D. The drug can have a metabolite that undergoes both hydroxylation and demethylation.
E. The majority of Bosentan's activity is done by the parent unmetabolized molecule and 20% comes from the active metabolite.
B, C, D, E
What are the functional groups circled here?
A. Red: Pyrimidine, Blue: Sulfonamide
B. Red: Sulfonamide, Blue: Pyrimidine
C. Red: Sulfonamide, Blue: Pyradine
D. Red: Sulfamide, Blue: Pyrimidine
What is the major possible side effect of Bosentan?
A. Liver Injury & Tetratogenicity
B. Kidney failure
D. CNS damage
Of the following drugs which of them is specific for ET-1 A type receptors?
A. Bosentan (Tracleer)
B. Macitentan (Opsumit)
C. Riosiguat (Adempas)
D. Ambrisentan (letaris)
Based on the structure of Ambrisenten, the blue group is a _____ and the red group is a _____
A. Carboxylic Acid, Pyradine
B. Ester, Pyrimidne
C. Carboxylic Acid, Pyrimidne
D. Ester, Pyradine
What statements about Ambrisentan are true? (Select All)
A. Contains a carboxylic acid and Pyrimidine functional group
B. Has a much higher affinity for ET-1 B receptors than ET-1 A receptors.
C. Has a possible chance to cause Liver injury and tetratogenicity
D. Has the potential to become soluble at lower pHs due to having a low pKa of 4
E. has the potential to become more soluble at higher pHs due to having a low pKa of 4
A, C, E
What kind of reaction can this functional group in ambrisentan undergo?
C. Ester hydrolysis
What kind of reaction can this group in Ambrisentan undergo?
What kind of reaction can this group undergo in ambrisentan?
B. Ester hydrolysis
C. Ether hydrolysis
The two methyl groups can undergo ____ and then undergo a second reaction known as ____
A. COMT, Glucuronidation
B. Hydroxylation, Glucuronidation
C. COMT, Sulfation
D. Hydroxylation, Sulfation
The following structure of Macitentan (Opsumit) includes all of the following EXCEPT:
Do not get the sulfonamide group confused with the sulfamide group. Sulfonamide only has one nitrogen and sulfamide has 2.
Which of the following drugs is non-selective to ET-1 A and ET-1 B receptors? (Select All)
A. Ambrisentan (Letairis)
B. Macitentan (Opsumit)
C. Bosentan (Tracleer)
Macitenten undergoes ____ to form an ____ metabolite
A. N-dealkylation, Inactive
B. N-dealkylation, Active
Nitric oxide ____ sGC in order to ____ levels of cGMP and promote muscle _____
A. Activates, Increase, Relaxation
B. Activates, Increase, Contraction
C. Deactivates, Decrease, Relaxation
D. Deactivates, Decrease, Contraction
When nitric oxide is placed in an _____ environment it will form the _____ which is capable of the shift in bonds known as _____
A. Aqueous, Nitrous Ion, Resonance
B. Aqueous, Nitrate Ion, Metabolism
C. Aqueous, Nitrate Ion, Resonance
D. Hydrophibic, Nitrate Ion, Resonance
What enzyme is sildenafil blocking that is preventing cGMP from being converted into GMP?
The boxed structure of Sildenafil is a ____ and is thus known as a ____.
A. Pyrimadine, Pyrimadine derivative
B. Indole, Indoline derivative
C. Pyrazole, Pyrazoline derivative
D. Purine, Purine derivative
All of the following statments are true about Sildenafil Citrate (Revatio) EXCEPT:
A. Sildenafil is a PDE5 inhibitor
B. Undergoes extensive presystemic metabilism (intestinal and first pass metabolism)
C. Keeps cAMP levels high within the muscle to promote muscle relaxation
D. Sildenafil is a purine derivative
Sildenafil keeps cGMP levels elevated not cAMP.
Which of the following statments is true regarding the metabolism of sildenafil?
A. Sildenafil undergoes N-dealkylation to produce an N-desmethyl metabolite
B. Sildenafil's N-desmethyl metabolite is 50% as potent as the parent compound.
C. The vast majority of sildenafil's activity comes from the parent compound.
D. All of the above
What two reactions can metabolite of tadalafil undergo? (Select All)
Which of the following hydroxyls can undergo COMT metabolism?
What kind of CYP3A4 reaction is occuring here?
B. Ether Hydrolysis
C. Ester Hydrolysis
Which hydroxyl group can undergo O-Glucuronidation?
T/F Metabolites formed by Tadalafil are all inactive