11C-labeled and18F-labeled PET ligands for subtype-specific imaging of histamine receptors in the brain

摘要: The signaling molecule histamine plays a key role in the mediation of immune reactions, gastric secretion, and sensory system. In addition, it has an important function as neurotransmitter central nervous system, acting pituitary hormone wakefulness, motor cognitive functions, well itch nociception. This raised interest histaminergic system for treatment diagnosis various pathologies such allergy, sleeping eating disorders, neurodegeneration, neuroinflammation, mood pruritus. In past 20 years, several ligands targeting four different receptor subtypes have been explored potential radiotracers positron emission tomography (PET). contribution provides overview developments subtype-selective carbon-11-labeled fluorine-18-labeled compounds imaging brain. Using specific radioligands, H1R expression human brain could be examined diseases schizophrenia, depression, anorexia nervosa. sedative effects antihistamines investigated terms occupancy. H3R is special because its regulatory release other neurotransmitters, initial PET studies humans reported. H4R youngest member family involved neuroinflammation pathways. To date, two H4R-specific 11C-labeled synthesized, vivo early stage.