IDENTIFICATION AND CHEMICAL SYNTHESIS OF MDL-105,212, A NONPEPTIDE TACHYKININ ANTAGONIST WITH HIGH-AFFINITY FOR NK1 AND NK2 RECEPTORS

Authors
BURKHOLDER TP KUDLACZ EM LE TB KNIPPENBERG RW SHATZER SA MAYNARD GD WEBSTER ME HORGAN SW
Citation
Tp. Burkholder et al., IDENTIFICATION AND CHEMICAL SYNTHESIS OF MDL-105,212, A NONPEPTIDE TACHYKININ ANTAGONIST WITH HIGH-AFFINITY FOR NK1 AND NK2 RECEPTORS, Bioorganic & medicinal chemistry letters, 6(8), 1996, pp. 951-956
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
8
Year of publication
1996
Pages
951 - 956
Database
ISI
SICI code
0960-894X(1996)6:8<951:IACSOM>2.0.ZU;2-S
Abstract
We have synthesized and identified MDL 105,212, a non-peptide tachykin in 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 1 05,212 and the SAR of a series of racemic amide analogs are described. Copyright (C) 1996 Elsevier Science Ltd