Neurotransmitters are endogenous chemicals that enable communication between neurons. Specifically, neurotransmitters are the brain chemicals that help relay messages from one part of the brain to another and between the brain and the rest of the body, primarily through synaptic transmission, also referred to as neurotransmission. The signals sent by neurotransmitters are responsible for the vast majority of brain and motor functions, including memory, planning, heart rate, respirations, digestion, hormonal responses, movement, and others. Many different diseases involve increased or decreased levels of neurotransmitters in the brain, which lead to different clinical features. Understanding the role of neurotransmitters and receptors in the brain is essential to gain insights into the neural bases of critical brain functions and pathological conditions, such as anxiety, depression, schizophrenia, Parkinson’s disease, drug addiction, learning problems, and many more. This chapter will provide an overview of (a) the different types of neurotransmitters and their functions, (b) the fundamental mechanisms of neuronal excitability, (c) signal generation and transmission, (d) synaptic transmission, (e) neural plasticity, (f) different types of receptors, and (g) the different illnesses and medications that target these receptors.