Endocannabinoid system has attracted the researchers to investigate into its ever fascinating roles governing many of the physiological functions in the human body. The prime endogenous cannabinoids are arachidonoylethanolamide also called anandamide and 2-arachidonoylglycerol. Recent pharmacological advances point out that this system of molecules are in initial stages and by updating our current knowledge, we could innovatively design molecules for suitable interventions that could be potentially beneficial to the mankind.