846060-68-2Relevant academic research and scientific papers
Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists
Cho, Kaimei,Ando, Makoto,Kobayashi, Kensuke,Miyazoe, Hiroshi,Tsujino, Toshiaki,Ito, Sayaka,Suzuki, Tomoki,Tanaka, Takeshi,Tokita, Shigeru,Sato, Nagaaki
scheme or table, p. 4781 - 4785 (2010/07/06)
A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K+ channel and serotonin transporter.
CYCLOPROPYL DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
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Page/Page column 63, (2010/02/10)
The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Burkholder, Timothy P.,Kudlacz, Elizabeth M.,Maynard, George D.,Liu, Xiao-Gao,Le, Tieu-Binh,Webster, Mark E.,Horgan, Stephen W.,Wenstrup, David L.,Freund, David W.,Boyer, Fred,Bratton, Larry,Gross, Raymond S.,Knippenberg, Robert W.,Logan, Deborah E.,Jones, Bryan K.,Chen, Teng-Man,Geary, Julie L.,Correll, Melinda A.,Poole, J. Chuck,Mandagere, Arun K.,Thompson, Thomas N.,Hwang, Kin-Kai
, p. 2531 - 2536 (2007/10/03)
We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors. Here we report the synthesis and structure-activity relationships for a series of analogs of MDL 105,212 with regards to: NK1 and NK2 receptor binding affinity, physical-chemical characterization; in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration.
