Medicinal Chemistry of Drugs Affecting Cardiovascular and Endocrine Systems

Ca+2 Channel Blockers

Author(s): Taufiq Rahman and M. O. Faruk Khan *

Pp: 40-69 (30)

DOI: 10.2174/9789815179729124030005

* (Excluding Mailing and Handling)


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.

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