Cannabinoids are chemicals that can be endogenous, natural, and synthetic substances which has the ability to bind to the cannabinoid receptors and exhibit a plethora of pharmacological and toxicological effects. Cannabinoids, the multipotent substance has a well-defined cellular signaling pathway that leads to a diverse physiological action in the body. Based on their chemical structural attributes, these substances can cross the blood–brain barrier, and hence, can exert an effect both in the central nervous system and the peripheral system in the body. Manipulation of the cannabinoid signaling with the natural and/or synthetic ligands can result in a plethora of pharmacological effects that can be used for various prophylactic and therapeutic treatment strategies in animals and humans. However, cannabinoids also induce severe adverse effects in the central and peripheral nervous systems. Hence, in this chapter, we review the current neuropharmacological and neurotoxicological properties of cannabinoids.