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Pharmaceuticals
Special Issues
Recent Advancements in Radiochemistry and PET Radiotracer Development: 2nd Edition
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Recent Advancements in Radiochemistry and PET Radiotracer Development: 2nd Edition

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: 25 August 2025 | Viewed by 1068

Special Issue Editors

Dr. Kenneth Dahl

E-Mail Website1 Website2
Guest Editor
1. PET Science Centre, Precision Medicine and Biosamples, Oncology R&D, AstraZeneca, Karolinska Institutet, SE-17176 Stockholm, Sweden
2. Department of Clinical Neuroscience, Centre for Psychiatry Research, Karolinska Institutet and Stockholm County Council, SE-17176 Stockholm, Sweden
Interests: PET; radiochemistry; automation; radioligand; drug discovery
Special Issues, Collections and Topics in MDPI journals
Dr. Sangram Nag

E-Mail Website
Guest Editor
Department of Clinical Neuroscience, Center for Psychiatry Research, Karolinska Institutet and Stockholm County Council, 17164 Stockholm, Sweden
Interests: PET; radioligand; neuroscience
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Positron Emission Tomography (PET) is a valuable imaging technique used in various applications, including clinical diagnosis, drug discovery, and neuroscience research. PET relies upon the administration of a chemical probe, also known as a radiotracer, which is labelled with a short-lived positron-emitting radionuclide (e.g., 11C, 18F, 68Ga, and 89Zr). The development of novel radiotracers requires multiple considerations, and aspects like radionuclide selection, labeling position, metabolic stability, precursor synthesis, radiolabeling procedure, automation, quality control, and regulatory aspects have to be considered.

This Special Issue aims to highlight the latest research on PET radiotracer synthesis and development, and we invite both original research and review articles on the following topics: (1) new radiolabeling strategies and isotopes for radiotracer production; (2) automation and clinical validation; (3) design and synthesis of novel PET radiotracers targeting specific biological processes, e.g., receptors, enzymes, and transporters; (4) strategies to enhance image quality and quantification; and (5) clinical translations and applications of novel PET radiotracers.

Overall, this Special Issue will provide an authoritative and up-to-date resource for researchers, clinicians, and industry professionals seeking to advance PET imaging and its applications in healthcare and biomedical research.

Dr. Kenneth Dahl
Dr. Sangram Nag
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • radiochemistry
  • labeling
  • automation
  • GMP
  • PET
  • radiotracer
  • radioligand
  • radiopharmaceutical
  • drug discovery

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Published Papers (1 paper)

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Research

9 pages, 3534 KiB  
Article
Radiolabeling and Preliminary In Vivo Evaluation of the Candidate CCR2 Targeting PET Radioligand [11C]AZD2423
by Kenneth Dahl, Peter Johnström, Miklós Tóth, Martin Bolin, Katarina Varnäs, Ryuji Nakao, Akihiro Takano, Yasir Khani Meynaq, Malken Bayrakdarian, Zsolt Cselényi, Christer Halldin, Lars Farde and Magnus Schou
Pharmaceuticals 2025, 18(2), 135; https://doi.org/10.3390/ph18020135 - 21 Jan 2025
Viewed by 770
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 [...] Read more.
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, t1/2 = 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 distribution. Results: Radiolabeling of [11C]AZD2423 was accomplished with good yield (7.4 ± 0.6%, n = 4) and high radiochemical purity (>99%) using [11C]carbon monoxide. Preliminary PET imaging in NHPs revealed low [11C]AZD2423 brain exposure under both baseline and pretreatment conditions (SUVpeak = 0.4, n = 2). However, high concentrations of radioactivity were observed in organs outside the brain at baseline, e.g., the thyroid gland (SUVpeak = 3.3, n = 2), parotid gland (SUVpeak = 3.4, n = 2), and submandibular gland (SUVpeak = 4.4, n = 2). This radioactivity was markedly reduced following pretreatment with AZD2423 (3.0 mg/kg), indicating specific binding of [11C]AZD2423 to CCR2 in vivo. The presence of specific CCR2 binding was further validated using two-tissue compartment modeling, which demonstrated a 59–63% reduction in the total volume of distribution values in the analyzed peripheral tissues. Conclusions: Altogether, [11C]AZD2423 shows potential as a PET radioligand for the in vivo visualization of CCR2 expression in tissues outside the brain and may also serve as a lead compound for the further development of a CCR2 PET radioligand suitable for brain imaging. Full article
(This article belongs to the Special Issue Recent Advancements in Radiochemistry and PET Radiotracer Development: 2nd Edition)
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