Radiolabeling and Preliminary In Vivo Evaluation of the Candidate CCR2 Targeting PET Radioligand [¹¹C]AZD2423.

ABSTRACT:

Background

AZD2423 is a high-affinity and selective negative allosteric modulator of the chemokine receptor type 2 (CCR2). This receptor plays important roles in the extravasation and transmigration of monocytes under inflammatory conditions. The aims of the current positron emission tomography (PET) study were as follows: (i) to develop an efficient synthetic method for labeling AZD2423 with carbon-11 (¹¹C, t_1/2 = 20.4 min) and (ii) to evaluate its potential to visualize CCR2 binding in the non-human primate (NHP) brain.

Methods

[¹¹C]AZD2423 was synthesized using a novel two-step, two-pot [¹¹C]carbon monoxide carbonylation procedure. PET imaging studies in NHPs (n = 2) were conducted to assess its brain penetration and in vivo dis

SUBMITTER: Dahl K 

PROVIDER: S-EPMC11858205 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature