BMY 7378, a selective α 1D -adrenoceptor antagonist, is a new angiotensin converting enzyme inhibitor: In silico, in vitro and in vivo approach

• Published in: Biochimica et biophysica acta. General subjects Vol. 1869; no. 1; p. 130732
• Main Authors: Rodríguez, Jessica E, Andrade-Jorge, Erik, Barquet-Nieto, Alina, Estrada-Soto, Samuel E, Gallardo-Ortíz, Itzell A, Villalobos-Molina, Rafael
• Format: Journal Article
• Language: English
• Published: Netherlands 01.01.2025
• Subjects: Adrenergic alpha-Antagonists - pharmacology; Adrenergic alpha-Antagonists - therapeutic use; Angiotensin-Converting Enzyme Inhibitors - pharmacology; Angiotensin-Converting Enzyme Inhibitors - therapeutic use; Animals; Captopril - pharmacology; Captopril - therapeutic use; Catalytic Domain - drug effects; Computer Simulation; Disease Models, Animal; Hypertension - drug therapy; Hypertension - metabolism; Inhibitory Concentration 50; Male; Molecular Docking Simulation; Myocardium - metabolism; Peptidyl-Dipeptidase A - analysis; Peptidyl-Dipeptidase A - metabolism; Piperazines - pharmacology; Piperazines - therapeutic use; Rats; Rats, Inbred SHR; Rats, Inbred WKY; Receptors, Adrenergic, alpha-1 - metabolism; Hypertension; α(1D)-AR; Spontaneously hypertensive rats; Molecular docking; Angiotensin converting enzyme

BMY 7378 is a multitarget drug primarily known for its selective antagonism of α -adrenoceptors (α -AR), exhibiting both hypotensive effects and the ability to prevent or reverse angiotensin II-induced vascular hypertrophy. Notably, BMY 7378 contains a phenylpiperazine moiety, a structural feature a...