In vitro studies using the Radiobiology and Bioimaging capabilities can assess a novel radiotracer’s affinity, selectivity, preliminary in vitro stability and metabolism in S9 (Phase I and II metabolisms) and microsomal (Phase II metabolism) fractions to predict how the radiotracer is absorbed, distributed, metabolised and excreted.
Many different pharmacological parameters of a radiotracer can be determined in different types of in vitro studies such as Saturation Receptor Binding studies (Dissociation constant Kd, Maximum receptor density Bmax), Inhibition Receptor Binding studies (Inhibition constant Ki or 50% Inhibition Concentration, IC50), Kinetic Receptor Binding studies (Association Rate constant Kon, Dissociation Rate constant Koff) in purified proteins, homogenate membrane fractions, subcellular fractions or whole cells to evaluate the characteristics and pharmacological profile of radiotracers.
Levels of radiotracer uptake can also be determined in cells to understand the mechanism of radiotracer transport into the cells. Selectivity or specificity studies can be undertaken to complete the pharmacological profile of a radiotracer.
- Radioligand uptake
- Radioligand binding (saturation, inhibition, kinetics, selectivity, specificity)
- In vitro metabolism
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