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The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets.
Tattersall FD, Rycroft W, Cumberbatch M, Mason G, Tye S, Williamson DJ, Hale JJ, Mills SG, Finke PE, MacCoss M, Sadowski S, Ber E, Cascieri M, Hill RG, MacIntyre DE, Hargreaves RJ. Tattersall FD, et al. Neuropharmacology. 2000 Feb 14;39(4):652-63. doi: 10.1016/s0028-3908(99)00172-0. Neuropharmacology. 2000. PMID: 10728886
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Ladduwahetty T, Baker R, Cascieri MA, Chambers MS, Haworth K, Keown LE, MacIntyre DE, Metzger JM, Owen S, Rycroft W, Sadowski S, Seward EM, Shepheard SL, Swain CJ, Tattersall FD, Watt AP, Williamson DW, Hargreaves RJ. Ladduwahetty T, et al. Among authors: cascieri ma. J Med Chem. 1996 Jul 19;39(15):2907-14. doi: 10.1021/jm9506534. J Med Chem. 1996. PMID: 8709125
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.
Stevenson GI, Huscroft I, MacLeod AM, Swain CJ, Cascieri MA, Chicchi GG, Graham MI, Harrison T, Kelleher FJ, Kurtz M, Ladduwahetty T, Merchant KJ, Metzger JM, MacIntyre DE, Sadowski S, Sohal B, Owens AP. Stevenson GI, et al. Among authors: cascieri ma. J Med Chem. 1998 Nov 5;41(23):4623-35. doi: 10.1021/jm980376b. J Med Chem. 1998. PMID: 9804702
High affinity phenylglycinol-based NK1 receptor antagonists.
Owens AP, Harrison T, Moseley JD, Swain CJ, Sadowski S, Cascieri MA. Owens AP, et al. Among authors: cascieri ma. Bioorg Med Chem Lett. 1998 Jan 6;8(1):51-6. doi: 10.1016/s0960-894x(97)10163-9. Bioorg Med Chem Lett. 1998. PMID: 9871627
135 results