Identification of the allosteric P2X₇ receptor antagonist [¹¹C]SMW139 as a PET tracer of microglial activation.

ABSTRACT: The P2X₇ receptor plays a significant role in microglial activation, and as a potential drug target, the P2X₇ receptor is also an interesting target in positron emission tomography. The current study aimed at the development and evaluation of a potent tracer targeting the P2X₇ receptor, to which end four adamantanyl benzamide analogues with high affinity for the human P2X₇ receptor were labelled with carbon-11. All four analogues could be obtained in excellent radiochemical yield and high radiochemical purity and molar activity, and all analogues entered the rat brain. [¹¹C]SMW139 showed the highest metabolic stability in rat plasma, and showed high binding to the hP2X₇ receptor in vivo in a hP2X₇ receptor overexp

SUBMITTER: Janssen B 

PROVIDER: S-EPMC5920098 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature