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Eplerenone, sold under the brand name Inspra, is an aldosterone antagonist type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for people with resistant hypertension due to elevated aldosterone.
Eplerenone is a newer drug that was developed as a spironolactone analog with reduced adverse effects. In addition to the y-lactone ring and the substituent on C-7, eplerenone has a 9α,11α-epoxy group. This group is believed to be the reason why eplerenone has a 20-40-fold lower affinity for the mineralocorticoid receptor than spironolactone. [7]
In modern computational chemistry, pharmacophores are used to define the essential features of one or more molecules with the same biological activity. A database of diverse chemical compounds can then be searched for more molecules which share the same features arranged in the same relative orientation.
Finerenone, marketed under the brand name Kerendia among others, is a medication used to reduce the risk of kidney function decline, kidney failure, cardiovascular death, non-fatal heart attacks, and hospitalization for heart failure in adults with chronic kidney disease associated with type 2 diabetes. [8]
Selexipag, sold under the brand name Uptravi, is a medication developed by Actelion for the treatment of pulmonary arterial hypertension (PAH). [3] [4] Selexipag and its active metabolite, ACT-333679 (or MRE-269, the free carboxylic acid), are agonists of the prostacyclin receptor, which leads to vasodilation in the pulmonary circulation. [5]
NADPH oxidase is an enzyme that effectively reduces O 2 to superoxide (O 2 –•), which can be used by the immune system to kill bacteria and fungi.Apocynin is an inhibitor of NADPH oxidase activity and thus is effective in preventing the production of the superoxide in human agranulocytes or neutrophilic granulocytes.
The exact mechanism of action of novaluron has not been extensively researched, but the general mechanisms and effects common to benzoylphenyl ureas apply. The compound inhibits chitin formation, targeting specifically larval insect stages that actively synthesize chitin. The adults of non-target species are seldom affected. [7]
Apararenone (developmental code name MT-3995) is a nonsteroidal antimineralocorticoid which is under development by Mitsubishi Tanabe Pharma for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.