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Lisinopril, one of the main comparators, is not a brain penetrant, although whether brain penetration increases with dementia is unknown.
Also, their brain penetration has been assessed (PAMPA-BBB assay).
Notably there was no apparent brain penetration of radiolabelled metabolites and no defluorination.
11 C]GSK931145 demonstrated good brain penetration and usefulness for GlyT1 occupancy study in monkeys [21].
Brain penetration of the ligand did not increase after P-gp and BCRP blockade.
Brain penetration is lower for other kynurenine metabolites (reviewed by Schwarcz et al., [19]).
For PD treatment, limited brain penetration of drug is a major concern.
Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
A pharmacokinetic study of compound 1 in vivo revealed good bioavailability and brain penetration in rats.
As a representative example, radiolabeled 6 was examined in vivo and showed reasonable brain penetration.
The receptor occupancy test in the rat cortex revealed favorable brain penetration of these compounds.
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