This chapter is a comprehensive account of medicinal chemistry of drugs
affecting the adrenergic system. It provides the mechanisms of action of drugs and
detail of structure-activity relationships of the adrenergic drugs to give the knowledge
base for pharmacists. After the study of this chapter students will be able to:
• Comprehend the historical background of adrenergic neurochemistry and drugs acting
on this system
• Explain adrenergic neurotransmitters and their functions
• Classify adrenergic receptors and their structures and binding
• Discuss direct and indirect acting sympathomimetic (adrenergic agonists) and
sympatholytic (adrenergic antagonists) drugs
• Explain SAR for direct and indirect acting adrenergic receptor agonists and
antagonists
• Delineate the clinical significance of these classes of drugs
• Identify the discovery process of these agents
Keywords: Adrenergic agonists and antagonists, Adrenergic drugs, Clinical use
of adrenergic drugs, Drug receptor interaction, Epinephrine and norepinephrine,
Structure activity relationship, Sympathomimetic agents.
