Publications by authors named "Marina T Macdonald-Soccorso"
Article Synopsis
- Gabapentin is an anticonvulsant drug that targets the α2δ subunit of calcium channels and is commonly used for neuropathic pain and epilepsy treatment.
- The study introduces two radiofluorinated forms of gabapentin, which can accumulate in injured nerves, and explores their potential for imaging α2δ receptors in the brain using advanced PET imaging in primates.
- Results show that while one derivative has low brain uptake and cannot be displaced, the other has moderate uptake and can be partially displaced, suggesting valuable insights into gabapentinoids’ mechanisms and future imaging applications.
Gabapentin, a selective ligand for the α2δ subunit of voltage-dependent calcium channels, is an anticonvulsant medication used in the treatment of neuropathic pain, epilepsy and other neurological conditions. We recently described two radiofluorinated derivatives of gabapentin (4-[F]fluorogabapentin, [F]tGBP4F, and 4-[F]fluorogabapentin, [F]cGBP4F) and showed that these compounds accumulate in the injured nerves in a rodent model of neuropathic pain. Given the use of gabapentin in brain diseases, here we investigate whether these radiofluorinated derivatives of gabapentin can be used for imaging α2δ receptors in the brain.
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- [F]3F4AP is a new PET radiotracer that targets potassium channels and shows potential for imaging neurological diseases, specifically demyelinated lesions, in animal studies, prompting its evaluation in humans for safety and radiation dosimetry.
- In a study with four healthy volunteers, the radiotracer was administered and monitored through a 4-hour dynamic PET scan, revealing the tracer's highest concentrations in organs like the kidneys, liver, and brain, with rapid clearance from the body.
- The average effective dose of radiation exposure from [F]3F4AP in humans was determined to be lower than in previous animal studies, and the safety findings showed no significant adverse effects