N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.

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Elliott JM, Carling RW, Chambers M, Chicchi GG, Hutson PH, Jones AB, MacLeod A, Marwood R, Meneses-Lorente G, Mezzogori E, Murray F, Rigby M, Royo I, Russell MG, Sohal B, Tsao KL, Williams B

N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5748-51. Epub 2006 Sep 6.

PubMed ID

16950620 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Talnetant	Neuromedin-K receptor	IC 50 (nM)	2.4	N/A	N/A	Details