Abstract
We wished to identify a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis. We aimed for compounds with low permeability, high solubility, that were substrates for the BBB efflux transporters MDR-1 and BCRP. The key lead PF-0868087 demonstrated over a 10-fold CNS-sparing profile in 2 preclinical species.
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