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ID: ALA1800009

Journal: Bioorg Med Chem Lett

Title: Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.

Authors: Myatt JW, Healy MP, Bravi GS, Billinton A, Johnson CN, Matthews KL, Jandu KS, Meng W, Hersey A, Livermore DG, Douault CB, Witherington J, Bit RA, Rowedder JE, Brown JD, Clayton NM.

Abstract: Optimization of the novel alpha-2-delta-1 ligand 4 provided compounds 37 and 38 which have improved DMPK profiles, good in vivo analgesic activity and in vitro selectivity over alpha-2-delta-2. An in-house P-gp prediction programme and the MetaSite software package were used to help solve the specific problems of high P-gp efflux and high in vivo clearance.

CiteXplore: 20566291

DOI: 10.1016/j.bmcl.2010.05.026