Bioorganic and Medicinal Chemistry Letters p. 2531 - 2536 (1997)
Update date:2022-08-05
Topics:
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
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.
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