30:718:409 Lecture 16: Antihypertensive Agents

• School: Rutgers University
• Department: Pharmacology and Toxicology
• Course: 30:718:409
• Professor: Dr. Lavoie and Dr. Chakalamanil

Document Summary

Adrenergic blockers, ( 1-selective and agents with isa preferred) Propranolol, pindolol, labetalol, carteolol, penbutolol, acebutolol, atenolol, etc. Structures for most are outlined within adrenergic antagonists. [kidneys: tumors in the adrenal medulla (pheochromocytoma, tumors in the adrenal cortex (mineralocorticoid effects, essential hypertension (etiology unresolved, renal hypertension (renin-angiotensin system) Types of hypertension: angiotensin-converting enzyme inhibition as a target in treating hypertension. Angiotensin amide is synthetic: used to see if people were super-sensitive to angiotensin ii. Saralin has affinity to angiotensin ii receptor and antagonizes it. An understanding of the mechanism of action of carboxypeptidase a provided a valuable lead in the development of ace inhibitors. The illustration above represents a model of the mode of action of carboxypeptidase a of bovine pancreas with a substrate protein and with an inhibitor. Note that there is a binding pocket for the substituent on the terminal amino acid and there is a cationic binding site for the terminal carboxylate.