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The present issue of Current Drug Targets is about bioactive phenothiazines, which have been both experimentally used or tested as drugs for treating or improving conditions in some diseases in various branches of medicine. The issue mainly concerns, how phenothiazine's molecular features could play a role of therapeutic nature and the side effects phenothiazines could produce. The volume also provides the general introductions to the topics in each chapter, with the intention that the researchers easily understand the current knowledge of each phenothiazine region. It contains information from both basic and preclinical investigations, highlighting the selectivity of their pharmacokinetic and metabolic processes. I strongly hope that the issue provides information to anyone who seeks to know more details about basic and therapeutic phenothiazines. The credit however, is shared by the various contributor's who conducted these studies as an international teamwork, focusing their researches on the phenothiazines. I thank all contributors of review papers of the phenothiazine's special issue from the bottom of my heart and it is hoped that the issue will serve as a stimulus for both further researchers and research studies in the phenothiazine therapeutics region.