1,2,4-TRIACYLPIPERIDINE SUBSTANCE-P ANTAGONISTS - SEPARATION OF AFFINITIES FOR THE NK-1 RECEPTOR AND THE L-TYPE CALCIUM-CHANNEL

Authors
MILLS SG MACCOSS M CASCIERI MA SADOWSKI S PATEL S CHAPMAN KL HUTSON PH
Citation
Sg. Mills et al., 1,2,4-TRIACYLPIPERIDINE SUBSTANCE-P ANTAGONISTS - SEPARATION OF AFFINITIES FOR THE NK-1 RECEPTOR AND THE L-TYPE CALCIUM-CHANNEL, Bioorganic & medicinal chemistry letters, 5(6), 1995, pp. 599-604
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
6
Year of publication
1995
Pages
599 - 604
Database
ISI
SICI code
0960-894X(1995)5:6<599:1SA-SO>2.0.ZU;2-L
Abstract
A series of 1,2,4-triacylpiperidines are shown to be potent antagonist s of the NK-1 (Substance P) receptor with significant affinity for the L-type calcium channel as well. The latter property can be diminished by suitable substitution on the terminal nitrogen while maintaining g ood NK-1 receptor binding.