Synthesis and characterization of a new Positron emission tomography probe for orexin 2 receptors neuroimaging.

ABSTRACT: The orexin receptors (OXRs) have been involved in multiple physiological and neuropsychiatric functions. Identification of PET imaging probes specifically targeting OXRs enables us to better understand the OX system. Seltorexant (JNJ-42847922) is a potent OX₂R antagonist with the potential to be an OX₂R PET imaging probe. Here, we describe the synthesis and characterization of [¹⁸F]Seltorexant as an OX₂R PET probe. The ex vivo autoradiography studies indicated the good binding specificity of [¹⁸F]Seltorexant. In vivo PET imaging of [¹⁸F]Seltorexant in rodents showed suitable BBB penetration with the highest brain uptake of %ID/cc = 3.4 at 2 min post-injection in mice. The regional brain biodistribution analysis and blocking

SUBMITTER: Bai P 

PROVIDER: S-EPMC9050936 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature