Positron emission tomography (PET) is an imaging technique to monitor the delivery of tracers labeled with positron emitters ( 1 1 C, 1 3 N, 1 5 O and 1 8 F). A wide variety of probes have been labeled to measure biochemical and physiological parameters in the central nervous system (CNS), such as glucose and oxygen metabolism, protein synthesis, blood flow, and neurotransmitter receptor functions. The delivery of labeled compounds to the target tissue, which directly reflect the distribution and kinetics patterns, especially to the neurotransmitter receptors is modulated by several factors, such as regional cerebral blood flow (rCBF), peripheral metabolism, and neurotransmitter concentration in the synaptic cleft. These factors provide misunderstanding of the apparent results, which do not reflect the true state of the CNS. The present paper will summarize several factors that affect the delivery of labeled compounds related to the neurotransmitter receptors in the CNS.