The endocannabinoid system is an incredibly pervasive network, influencing the homeostasis of immune, cardiovascular, central nervous, and cutaneous systems, among many others. The biological effects of the endocannabinoid system were gleaned mostly from the natural source, the plant Cannabis sativa, native to Central Asia and the Indian subcontinent. The plant has been mostly exploited for its euphoriant and relaxant properties, however, the endocannabinoid system is slowly entering the forefront of pharmacotherapy of various clinical entities. The recent isolation of the functional endocannabinoid receptor led to the appreciation of the scope of intracellular signalling and the far-reaching genomic and non-genomic consequences of the cannabinoid receptor activation. This thesis aims to provide a well-rounded overview of the physiology of the endocannabinoid system, its role in the homeostasis of many functional systems in the body, a description of various potentially therapeutic ligands at the cannabinoid receptors, and the numerous opportunities which provide a glimpse into new avenues in drug discovery and development. The industry has attempted to devise novel therapeutic approaches to the endocannabinoid system in the past, however, successful molecules are rare and restricted to only a few clinical indications. The thesis will discuss the possible foci of application of new endocannabinoid targets and the clinical relevance of new, promising therapies.