One-step, kit-based radiopharmaceuticals for molecular SPECT imaging: a versatile diphosphine chelator for ^99mTc radiolabelling of peptides.

ABSTRACT: Radiotracers labelled with technetium-99m (^99mTc) enable accessible diagnostic imaging of disease, provided that radiotracer preparation is simple. Whilst ^99mTc radiopharmaceuticals for imaging perfusion are routinely prepared from kits, and regularly used in healthcare, there are no ^99mTc-labelled receptor-targeted radiopharmaceuticals in widespread clinical use. This is in part due to the multistep radiosyntheses required for the latter. We demonstrate that the diphosphine, 2,3-bis(diphenylphosphino)maleic anhydride (BMA), is an excellent platform for preparation of kit-based, receptor-targeted ^99mTc-labelled radiotracers: its conjugates are simple to prepare and can be easily labelled with ^99mTc using one-step, kit-based protocols.

SUBMITTER: Hungnes IN 

PROVIDER: S-EPMC8594432 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature