Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK 1 and NK 2 receptors

…, RW Knippenberg, SA Shatzer, GD Maynard…

Index: Burkholder, Timothy P.; Kudlacz, Elizabeth M.; Le, Tieu-Binh; Knippenberg, Robert W.; Shatzer, Scott A.; Maynard, George D.; Webster, Mark E.; Horgan, Stephen W. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 8 p. 951 - 956

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Citation Number: 40

Abstract

We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 (IC50= 3.11 nM) and NK2 (IC50= 8.40 nM) receptors. The chemical synthesis of MDL 105,212 and the SAR of a series of racemic amide analogs are described.