CVD WK8 angiotensin antagonist
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29 Terms
What is the common scaffold of ARBs?
Biphenyl tetrazole
What is the role of the tetrazole ring in ARBs?
Bioisostere for carboxylate
What is the key C-terminal amino acid for AT₁ binding?
Phe⁸
Why must ARBs be AT₁ selective?
To avoid blocking AT₂ (which has beneficial effects - vasodilation, anti-growth)
What is the IC₅₀ of losartan?
0.019 μM
What is the IC₅₀ of valsartan?
0.0089 μM
What is the IC₅₀ of irbesartan?
0.0013 μM
Which ARB has an imidazole ring?
Losartan
Which ARB is the most potent?
Irbesartan (IC₅₀ = 0.0013 μM)
Which ARB has a spiro ring system?
Irbesartan
Which ARB has a non-imidazole scaffold?
Valsartan
What is SOSA?
Selective Optimization of Side Activities - a medicinal chemistry technique
What is a bioisostere?
A group that mimics the function of another group but has different chemical properties
What is a peptidomimetic?
A molecule that mimics a peptide structure but is not a peptide
What was the first ARB?
Losartan
What company developed losartan?
Dupont
What company discovered the initial peptide mimic?
Takeda (1979)
What is the biphenyl tetrazole scaffold?
Two benzene rings connected, with a tetrazole ring attached - the core of ARBs
What is the difference between losartan and valsartan?
Losartan has imidazole; valsartan has non-imidazole scaffold
What is the difference between losartan and irbesartan?
Irbesartan has a spiro ring system and is more potent
What is the AT₁ receptor?
The receptor that mediates vasoconstriction, aldosterone release, sympathetic activation
What is the AT₂ receptor?
The receptor that mediates vasodilation, anti-growth, anti-fibrotic effects
What does AT₂ activation do?
Vasodilation, anti-growth, anti-fibrotic (opposes AT₁)
Why is AT₂ beneficial?
It opposes the harmful effects of AT₁
What is the sequence of angiotensin II?
Asp-Arg-Val-Tyr-Ile-His-Pro-Phe
What is the role of Phe⁸ in angiotensin II?
Critical for AT₁ receptor binding
What is the role of His⁶ in angiotensin II?
Important for AT₁ receptor binding (imidazole ring)
What is the difference between 1st and 2nd generation ARBs?
2nd generation has better potency, bioavailability, and duration
What is the active metabolite of losartan?
EXP-3174