GR159897 AND RELATED ANALOGS AS HIGHLY POTENT, ORALLY-ACTIVE NONPEPTIDE NEUROKININ NK2 RECEPTOR ANTAGONISTS

Authors
COOPER AWJ ADAMS HS BELL R GORE PM MCELROY AB PRITCHARD JM SMITH PW WARD P
Citation
Awj. Cooper et al., GR159897 AND RELATED ANALOGS AS HIGHLY POTENT, ORALLY-ACTIVE NONPEPTIDE NEUROKININ NK2 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(16), 1994, pp. 1951-1956
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
16
Year of publication
1994
Pages
1951 - 1956
Database
ISI
SICI code
0960-894X(1994)4:16<1951:GARAAH>2.0.ZU;2-C
Abstract
Optimisation of NK2 receptor affinity in a series of sulfur derivative s resulted in the identification of highly potent 5-fluoroindol-3-ylet hyl[4-(phenylsulfinyl methyl)]piperidines. Further structure activity analysis led to GR 159897 an NK2 receptor antagonist which potently bl ocks agonist-induced bronchoconstriction in the guinea-pig when admini stered by peripheral and oral routes.