Abstract

The cannabinoid system constitutes a key entity throughout the human body. The cannabinoid type 1 receptor (CB1R), the prominent cannabinoid component in the brain, interacts significantly with the dopaminergic system and its role in reward. CB1Rs have been implicated in “reward disorders” such as obesity and substance abuse, as well as in schizophrenia and mood disorders. The further exploration of the role of these receptors is important for a general knowledge of the brain and, ultimately, for the development of drugs to target associated diseases. Positron emission tomography (PET) imaging allows for the investigation of specific receptors in vivo. PET radioligands targeted to the specific receptor type are essential. The development of effective radiotracers for imaging CB1R has been met with challenges, due to poor blood brain permeability, nonspecificity and fast washout. The current chapter provides a review of the three CB1R PET radioligands available for use to investigate the cannabinoid system in humans in health and disease.

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