SYNTHESIS AND NK1 RECEPTOR ANTAGONISTIC ACTIVITY OF (+ CYL-3-(3,4-DICHLOROPHENYL)-3-[2-(SPIRO-SUBSTITUTED PIPERIDIN-1'-YL)ETHYL]PIPERIDINES/

Authors
KUBOTA H OKAMOTO Y FUJII M IKEDA K TAKEUCHI M SHIBANUMA T ISOMURA Y
Citation
H. Kubota et al., SYNTHESIS AND NK1 RECEPTOR ANTAGONISTIC ACTIVITY OF (+ CYL-3-(3,4-DICHLOROPHENYL)-3-[2-(SPIRO-SUBSTITUTED PIPERIDIN-1'-YL)ETHYL]PIPERIDINES/, Bioorganic & medicinal chemistry letters, 8(12), 1998, pp. 1541-1546
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
12
Year of publication
1998
Pages
1541 - 1546
Database
ISI
SICI code
0960-894X(1998)8:12<1541:SANRAA>2.0.ZU;2-M
Abstract
cyl-3-(3,4-dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl) et hyl]piperidines and their quaternary ammonium salts were prepared and evaluated for their NK1 receptor antagonistic activity. Some of these inhibited SP-induced contraction in guinea pig ileum with IC50 values at a level of 10(-9) M and showed potent inhibitory activity against s elective NK1 receptor agonist-induced bronchoconstriction in guinea pi gs, (C) 1998 Elsevier Science Ltd. All rights reserved.