Radiohalogens for PET Imaging

Enabling Efficient Positron Emission Tomography (PET) Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) with a Robust and One-Step Radiosynthesis of a Highly Potent 18F-Labeled Ligand ([18F]UCB-H)

“…The ubiquity of SV2A in the human brain, however, offers a unique opportunity to peek into the very mechanisms of neurotransmission and improve the understanding, diagnosis, and treatment of epilepsy and other neurological conditions using PET technology. PET has indeed become a cornerstone tool for (pre)­clinical research and routine diagnosis over the past decades; − with its convenient 110 min half-life, almost exclusive β + decay, and the significant representation of fluorine in pharmacologically active molecules, fluorine-18, in its no-carrier-added, nucleophilic ([ 18 F]­F – ) form, is one of the most practical nuclides currently in use for clinical PET imaging …”

Base‐Mediated Radio‐Iodination of Arenes by Using Organosilane and Organogermane as Radiolabelling Precursors

“…Radio-halogens are prevalent species in nuclear medicine due to their wide field of applications in molecular imaging and radiotherapy. [1][2][3][4][5][6] Thus, covalent bond formation between radiohalogens and relevant molecular substrates is a major topic in radiochemistry generally, achieved through transfer of standard halogenation reactions to radio-halogenation reactions. Several challenges arise when it comes to performing halogenation in a radiosynthetic context, such as limited chemical sources, extreme dilution of the radio-isotope, large excess of substrate and reagents, radiation protection and isotope half-lives (Scheme 1).…”

1-(N,N-Dialkylcarbamoyl)-1,1-difluoromethanesulfonyl ester as a stable and effective precursor for a neopentyl labeling group with astatine-211

“…Radiohalogens with a short half-life have been used as radioisotopes for radiopharmaceuticals. 2 For instance, fluorine-18 and iodine-123, as positron and single-photon emitters, respectively, allow for external visualization, thereby proving indispensable for diagnostic applications. In contrast, astatine-211, iodine-131, and bromine-77, which are alpha, beta, and Auger electron emitters, respectively, tend to damage surrounding cells, but can potentially be utilized for therapeutic purposes.…”