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ABC transporters P-gp and Bcrp do not limit the brain uptake of the novel antipsychotic and anticonvulsant drug cannabidiol in mice.
A positron emission topography (PET) study showed chronic schizophrenia patients had considerably lower brain uptake of the P-gp substrate 11C-verapamil in the temporal cortex, basal ganglia, and amygdala, but not in the thalamus or prefrontal cortex.
Moreover, competition studies with -nicotine (5 mg/kg, 5 min before the radiotracer injection) did not reduce brain uptake of the radiotracer.
The brain uptake of the IgG fusion proteins, 2 3% of injected dose/brain, is comparable to the brain uptake of small molecules.
Engineered binding affinity, avidity and pH-sensitivity have been shown to affect binding, intracellular sorting and release, ultimately leading to increased brain uptake of the targeting vector and its associated cargo.
A11 Influence of a genetic polymorphism on brain uptake of the dual ABCB1/ABCG2 substrate [11C]tariquidar.
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Even though the efficacy studies are preliminary, with dendrimer drug conjugates studied in a small number of animals, we focused on demonstrating the brain uptake of dendrimers and the therapeutic feasibility of this approach and on the reduction in adverse systemic side effects.
As for the two patients who had negligible brain uptake of VGB after the first dose, only Patient 4 still had minimal increase in microdialysate VGB concentration above baseline after the third dose, while Patient 2 showed a typical increase above baseline.
Because the proposed estimation method makes use of dose equivalent rates on the surface of the right temporal lobe, other factors, that may affect brain uptake of FDG and, consequently, the accuracy of the method, should be considered.
Despite several published studies, there is still an ongoing debate, whether P-gp inhibition with tariquidar or other inhibitors is enhancing the brain uptake of substrate radiotracers by increasing the influx or decreasing outflux across the BBB of the radiotracer [9].
In order to ascertain the brain uptake of 18F-nifene, after completion of the in vivo microPET scans, the rats were sacrificed and the brain was extracted for ex vivo microPET imaging.
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