| Literature DB >> 16950620 |
Jason M Elliott1, Robert W Carling, Mark Chambers, Gary G Chicchi, Peter H Hutson, A Brian Jones, Angus MacLeod, Rose Marwood, Georgina Meneses-Lorente, Elena Mezzogori, Fraser Murray, Michael Rigby, Inmaculada Royo, Michael G N Russell, Bindi Sohal, Kwei Lan Tsao, Brian Williams.
Abstract
A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properties.Entities:
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Year: 2006 PMID： 16950620 DOI： 10.1016/j.bmcl.2006.08.086
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823