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.

Keywords: Benzothiazepines (BTZs), Ca²⁺-channels, CCBs, Drug-receptor interaction, Dihydropyridines (DHPs), Dihydropyridine receptors (DHPR), Diaminopropanol ethers, Phenylalkylamines (PAAs), Structure-activity relationship (SAR), VGCC.