Ca⁺² Channel Blockers

Abstract

This chapter is a comprehensive account of the medicinal chemistry of antihypertensive drugs, Ca2+-channel blockers (CCBs). It provides the mechanism of drug action and detailed structure-activity relationships (SAR) of the CCBs to give the knowledge base for pharmacists. After studying this chapter, students will be able to: • Comprehend the historical background of the CCBs. • Classify different types of voltage-gated Ca2+ channels (VGCCs) and their clinical significance. • Explain CCBs and their clinical significance. • Describe the mechanisms of action of CCBs at the molecular level including their binding modes against the VGCCs. • Describe the SAR of the different classes of CCBs. • Delineate clinical significance and therapeutic evaluations of these classes of drugs by solving case studies. • Articulate the discovery process of a few CCBs.