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Protein Binding
Brain Tissue Binding
Brain-to-Plasma Distribution
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Ready-to-use assay systems for DMPK and ADMET studies

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Brain Tissue Binding

A fast high throughput Brain Absorption assay for estimation of brain tissue binding of drugs and the prediction of their disposition into the brain.

The assay is based on the affinity of compounds to brain membranes and provides an accurate estimation of the unbound fraction of drugs in brain and the brain-to-plasma distribution.

  • Ready-to-use 96-well microtiter plates carrying TRANSIL beads with a single lipid bilayer reconstituted from porcine brain lipids, designed to conveniently measure brain tissue binding and predicts blood-brain barrier penetration.
  • Includes spreadsheet, facilitating manipulation of statistical parameters and calculation of final results.
  • Designed for automated liquid handlers or manual pipetting.
  • TRANSIL bead s are integrated into a 96-well microtiter plates enable easy handling.
  • One plate can be used for measuring brain tissue binding and brain disposition of up to 12 compounds.
  • Only 12 minutes assay incubation time.
  • Rapid compound quantification due to immobilized plasma proteins (e.g. injection via RapidFire™).
  • Highly reproducible results and robust correlation with conventional dialysis technique.
Background and Technical Information

The TRANSIL Brain Absorption assay is used to assess the availability of drug in the central nervous system (CNS). Available as a kit, this assay eases the search for new CNS drugs and reduces the discovery costs significantly as shown through external validation. Before the introduction of this assay these tests could only be conducted in animal models or freshly prepared animal tissue in in vitro assays. Thus, the TRANSIL assay not only simplifies the discovery process by not requiring dissection of animals and tissue processing, it also reduces animal consumption and massively decreases the labor requirements to assess brain availability. Another application of this assay is the prediction of CNS side effects in all indication areas (e.g. headache, nausea, prolonged reaction times etc.) at a development stage where this knowledge can still be used to eliminate them.

For many years emphasis in CNS drug discovery has been placed on the magnitude of the brain to plasma ratio (B/P ratio or Kp), even though, in many cases, brain total concentration correlates poorly with a mechanistic pharmacodynamic response. Total drug concentration values in brain, measured by in vivo experiments or estimated with the hybrid model based on the brain membrane affinity (measured by the TRANSILXL Brain Absorption kit) and plasma protein binding (e.g. measured by the TRANSILXL PPB kit) are corrected for the fraction of drug unbound in brain which is estimated by the TRANSILXL Brain Absorption kit to obtain an estimate of the brain unbound concentration (Cu,brain). This has been successfully demonstrated across a range of CNS targets to yield a much better correlation between receptor occupancy and pharmacodynamic endpoints.

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