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Over the past decade, psychiatry has grown in close contact with the advancements of clinical neurosciences. In particular, basic and clinical psychopharmacology has largely benefited from a large array of neuroimaging studies, which provided a direct way of investigating the pathophysiology of mental disorders in vivo. The structural cerebral abnormalities of gray and white matter underlying the clinical features of schizophrenia and affective disorders, have been investigated respectively with Magnetic Resonance Imaging (MRI) and Diffusion Tensor Imaging (DTI). The function of neurotransmitters mostly implicated in major psychiatric illnesses, for example dopamine and glutamate, has been assessed by using molecular imaging techniques such as positron emission tomography (PET), single-photon emission tomography (SPET), and magnetic resonance spectroscopy (MRS). Regional brain activity associated with specific cognitive processes or symptoms underlying psychiatric disorders, has been studied by using functional magnetic resonance imaging methods (fMRI). Other advanced techniques have allowed researchers to investigate the connectivity patterns between different brain regions and integrate neuroimaging findings with electrophysiological measures. Overall, the potentials of neuroimaging methods in psychopharmacology are largely based on their promises to clarify the neurobiological substrates of psychiatric disorders and to assist clinicians in the diagnostic processes, as the core pathophysiological abnormalities that underlie these diseases have yet to be identified. This may, in turn, inform the discovery and the development of new medications for the treatment of psychiatric conditions. The review articles included in this issue of Current Pharmacological Design feature leaders in the field related to psychopharmacological neuroimaging. Focus is given to psychosis and affective disorders (bipolar disorder and major depression). The encompassing aim of this issue is to provide the readers working in basic biomedical science and the clinicians a comprehensive understanding of different neuroimaging techniques and their psychopharmacological applications.