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Issue 3, 2012
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The discovery and profile of PF-0868087, a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis

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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.

Graphical abstract: The discovery and profile of PF-0868087, a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis

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Publication details

The article was received on 01 Nov 2011, accepted on 25 Nov 2011 and first published on 30 Nov 2011


Article type: Concise Article
DOI: 10.1039/C2MD00276K
Citation: Med. Chem. Commun., 2012,3, 339-343
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    The discovery and profile of PF-0868087, a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis

    G. Lunn, C. E. Mowbray, W. L. S. Liu, V. M. Joynson, T. Hay and M. Yeadon, Med. Chem. Commun., 2012, 3, 339
    DOI: 10.1039/C2MD00276K

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