This chapter explains the intricate relationship between neurotransmission and exercise, which is crucial for exercise science. By exploring the role of neurotransmitters, we can shed light on their fundamental role and importance in understanding neurotransmission in exercise science and sports performance. Furthermore, this chapter engages in the basics of neurotransmission, emphasizing the importance of understanding these complex neurochemical processes within exercise. The narrative further delves into exercise components, highlighting the interplay of major neurotransmitter systems—dopamine, serotonin, noradrenaline, and glutamate—and their influence on exercise tolerance. Moreover, this chapter will provide readers with a comprehensive description of some of the most critical changes in neurotransmission associated with different forms of exercise. Particular emphasis is placed on exercise-related components such as modality, intensity, and complexity. By understanding the role of neurotransmitters in exercise science, individuals can better achieve their fitness goals and improve their overall health and well-being. This chapter provides an in-depth discussion of neurotransmission and exercise science, making it highly relevant for readers with an interest in exercise, fitness, and health.