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Antagonist G is a neuropeptide antagonist.1,2,3 It inhibits the binding of vasopressin to rat liver or Swiss 3T3 membranes (IC50s = 3.5 and 2.2 µM, respectively) and vasopressin-induced production of inositol phosphate in Swiss 3T3 fibroblasts (IC50 = 1 µM).1 Antagonist G (50 µM) induces apoptosis and the production of reactive oxygen species (ROS) in NCI H69 small cell lung cancer (SCLC) cells.2 It reduces tumor growth in an NCI H69 mouse xenograft model when administered at a dose of 45 µg/g.3

1.Seckl, M.J., Newman, R.H., Freemont, P.S., et al.Substance P-related antagonists inhibit vasopressin and bombesin but not 5’-3-O-(thio)triphosphate-stimulated inositol phosphate production in swiss 3T3 cellsJ. Cell Physiol.163(1)87-95(1995) 2.MacKinnon, A.C., Waters, C., Rahman, I., et al.[Arg6, D-Trp7,9, NmePhe8]-substance P (6-11) (antagonist G) induces AP-1 transcription and sensitizes cells to chemotherapyBr. J. Cancer.83(7)941-948(2000) 3.Langdon, S., Sethi, T., Ritchie, A., et al.Broad spectrum neuropeptide antagonists inhibit the growth of small cell lung cancer in vivoCancer Res.52(16)4554-4557(1992)

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