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Atenolol
6%
11/192
Carvedilol
28%
53/192
Esmolol
8%
15/192
Pindolol
20%
38/192
Propranolol
24%
46/192
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This antihypertensive drug that can either activate or inhibit beta-adrenergic receptors is most likely a partial beta-agonist, of which a classic example is the drug pindolol. Beta-blockers are a class of drugs that work by inhibiting the beta-adrenergic receptor. These receptors are found on cardiac myocytes and the sinoatrial node and normally increase the ionotropic and chronotropic properties of the heart. The molecular basis of this effect is that beta-adrenergic receptors are linked to the G-protein coupled receptor stimulatory subtype, which increases adenylyl cyclase activity, produces more cyclic adenosine monophosphate, and results in increased protein kinase A activity. Partial agonists such as acebutolol and pindolol can increase this activity in the absence of epinephrine and decrease this activity in the presence of epinephrine. Incorrect Answers: Answer 1 & 3: Atenolol and esmolol (very short half-life) are beta-1-selective antagonists; however, it would not have partial agonist activity and would never increase the level of cyclic adenosine monophosphate. Answer 2: Carvedilol is a nonselective alpha- and beta-antagonist; however, it would not have partial agonist activity and would never increase the level of cyclic adenosine monophosphate. Answer 5: Propranolol is a nonselective beta-antagonist; however it would not have partial agonist activity and would never increase the level of cyclic adenosine monophosphate. Bullet Summary: Acebutolol and pindolol are partial agonists at the beta-adrenergic receptor.
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