Title of article :
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
Author/Authors :
Timothy P. Burkholder، نويسنده , , Elizabeth M. Kudlacz، نويسنده , , Tieu-Binh Le، نويسنده , , Robert W. Knippenberg، نويسنده , , Scott A. Shatzer، نويسنده , , George D. Maynard، نويسنده , , Mark E. Webster، نويسنده , , Stephen W. Horgan، نويسنده ,
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.
