In this chapter, we will introduce you to the fascinating world of GPCRs. We will discuss their structure, function, and diversity, providing you with a solid foundation for understanding their role in drug discovery and development.

In this chapter, we will delve into the various physiological processes where GPCRs play a crucial role. We will explore the intricacies of their involvement in vision, olfaction, taste, and the regulation of cardiovascular, respiratory, and immune functions.

In this chapter, we will explore the mechanisms of action and therapeutic applications of FDA-approved drugs targeting GPCRs. We will discuss the various strategies used to target GPCRs, the advantages and limitations of these approaches, and real-world case studies illustrating their clinical utility.