Radiosynthesis, ex Vivo Biodistribution, and in Vivo Positron Emission Tomography Imaging Evaluations of [¹¹C]2-Pyridinealdoxime Methiodide ([¹¹C]2-PAM): A First-In-Class Antidote Tracer for Organophosphate Intoxication.

ABSTRACT: 2-Pyridinealdoxime methiodide (2-PAM) is a widely used antidote for the treatment of organophosphorus (OP) exposure that reactivates the target protein acetylcholinesterase. Carbon-11 2-PAM was prepared to more fully understand the in vivo mode of action, distribution, and dynamic qualities of this important countermeasure. Alkylation of 2-pyridinealdoxime with [¹¹C]CH₃I provided the first-in-class [¹¹C]2-PAM tracer in 3.5% decay corrected radiochemical yield from [¹¹C]CH₃I, >99% radiochemical purity, and 4831 Ci/mmol molar activity. [¹¹C]2-PAM tracer distribution was evaluated by ex vivo biodistribution and in vivo dynamic positron emission tomography (PET) imaging in naïve (OP exposure deficient) rats. Tracer alone and tra

SUBMITTER: Neumann KD 

PROVIDER: S-EPMC6699170 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature