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

Filomena Mattner,Andrew Katsifis,Thomas Bourdier, Christian Loc'h,Paula Berghofer, Christopher Fookes,Tzong-Tyng Hung,Timothy Jackson,David Henderson,Tien Pham,Brendan J. Lee,Rachael Shepherd,Ivan Greguric,Naomi Wyatt,Thanh Le,Jackson Poon,Carl Power,Michael Fulham

RSC Medicinal Chemistry（2021）

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摘要

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.

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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

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