Synthesis and pharmacological evaluation of [18F]PBR316: a novel PET ligand targeting the translocator protein 18 kDa (TSPO) with low binding sensitivity to human single nucleotide polymorphism rs6971-Reference-Cited by-同舟云学术

Synthesis and pharmacological evaluation of [18F]PBR316: a novel PET ligand targeting the translocator protein 18 kDa (TSPO) with low binding sensitivity to human single nucleotide polymorphism rs6971

Published:2021 Issue:7 Volume:12 Page:1207-1221
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Mattner Filomena¹²³⁴^ORCID,Katsifis Andrew¹²³⁴⁵^ORCID,Bourdier Thomas¹²³⁴^ORCID,Loc'h Christian⁶⁷⁴^ORCID,Berghofer Paula⁶⁷⁴^ORCID,Fookes Christopher⁶⁷⁴^ORCID,Hung Tzong-Tyng⁸⁹¹⁰⁴^ORCID,Jackson Timothy⁶⁷⁴^ORCID,Henderson David¹²³⁴^ORCID,Pham Tien⁶⁷⁴^ORCID,Lee Brendan J.⁸⁹¹⁰⁴^ORCID,Shepherd Rachael⁶⁷⁴^ORCID,Greguric Ivan⁶⁷⁴^ORCID,Wyatt Naomi⁶⁷⁴^ORCID,Le Thanh¹²³⁴^ORCID,Poon Jackson¹²³⁴^ORCID,Power Carl⁸⁹¹⁰⁴^ORCID,Fulham Michael¹²³⁴¹¹^ORCID

Affiliation:

1. Department of Molecular Imaging

2. Royal Prince Alfred Hospital

3. Camperdown

4. Australia

5. School of Pharmacy

6. Australian Nuclear Science and Technology Organisation

7. Lucas Heights

8. Biological Resources Imaging Laboratory

9. University of New South Wales

10. Sydney

11. Faculty of Engineering and Information Technologies

Abstract

PBR316 has high brain uptake, biodistribution consistent with TSPO expression and is insensitive to rs6971 polymorphism with a LAB:HAB ratio of 1.5. It can be prepared in >99% radiochemical purity, 160–400 GBq μmol⁻¹ and >98.5% stability after 4 h.

Funder

University of New South Wales

Australian Nuclear Science and Technology Organisation

Prostate Cancer Foundation of Australia

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/MD/D1MD00035G

Reference58 articles.

1. Current status and future perspectives: TSPO in steroid neuroendocrinology