Evaluation of Specific Binding of [11C]RTI-97 to Kappa Opioid Receptor by Autoradiography and PET Imaging in Rat.
Fabien FillesoyeMéziane IbazizèneNicolas MarieFlorence NobleCécile PerrioPublished in: ACS medicinal chemistry letters (2021)
Kappa opioid receptor (KOR) PET imaging remains attractive to understand the role of KOR in health and diseases and to help the development of drugs especially for psychiatric disorders such as depression, anxiety, and addiction. The potent and selective KOR antagonist RTI-97 labeled with carbon-11 was previously demonstrated to display specific KOR binding in mouse brain by ex vivo autoradiography studies. Herein, we evaluated [11C]RTI-97 in rat by in vitro autoradiography and by in vivo PET imaging. The radiosynthesis of [11C]RTI-97 was optimized to obtain high molar activities. Despite a low cerebral uptake, the overall results showed a heterogeneous repartition and specific KOR binding of [11C]RTI-97 in brain and a high and specific accumulation of [11C]RTI-97 in pituitary in accordance with KOR expression.
Keyphrases
- pet imaging
- positron emission tomography
- binding protein
- chronic pain
- healthcare
- pain management
- public health
- poor prognosis
- oxidative stress
- computed tomography
- depressive symptoms
- multiple sclerosis
- dna binding
- sleep quality
- resting state
- cerebral ischemia
- toll like receptor
- blood brain barrier
- climate change
- brain injury
- drug induced