Optimization of microtubule-stabilizing triazolopyrimidines as therapeutics for Alzheimer's disease and related tauopathies
$311,482U01FY2022AGNIH
University Of Pennsylvania, Philadelphia PA
Investigators
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Abstract
Statement of Work Specific activities overseen by the Brunden laboratory include: 1) testing of prodrugs in established HEK293 and neuron microtubule stabilization assays; 2) intravenous and oral pharmacokinetic testing of prodrugs to determine the rate of conversion of prodrugs to the desired active compound; 3) assessment of preferred prodrugs for pharmacodynamic effect in wild-type mice to establish the minimum effective dose and duration of compound effect; and 4) determination of preferred prodrug acute maximum tolerated dose and the no adverse effect dose after 3 weeks of dosing.
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