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Positron emission tomography (PET) neuroimaging in neuropsychiatry is a powerful tool for the quantification of molecular brain targets to characterize disease, assess disease subtype differences, evaluate short- and long-term effects of treatments, or even to measure neurotransmitter levels in healthy and psychiatric conditions. In this work, we present different methodological approaches (time-invariant models and models with time-varying terms) that have been used to measure dynamic changes in neurotransmitter levels induced by pharmacological or behavioral challenges in humans. The developments and potential use of hybrid PET/magnetic resonance imaging (MRI) for neurotransmission brain research will also be highlighted.