Issue 3, 2012
From the journal:

MedChemComm

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

Graham Lunn,*a   Charles E. Mowbray,a   Wai L. S. Liu,b   Valerie M. Joynson,b   Tanya Hayc  and  Michael Yeadonb  

* Corresponding authors

a Sandwich Chemistry, World Wide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich, UK
E-mail: grahamlunn40@yahoo.co.uk

b Allergy and Respiratory Research Unit, Pfizer, Ramsgate Road, Sandwich, UK

c DMPK, Pfizer, Ramsgate Road, Sandwich, UK

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

About
Cited by
Related
Download options Please wait...

Article information

DOI
https://doi.org/10.1039/C2MD00276K
Article type
Concise Article
Submitted
01 Nov 2011
Accepted
25 Nov 2011
First published
30 Nov 2011

Med. Chem. Commun., 2012,3, 339-343

Permissions

Request permissions

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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements