Linked Life Data

7540207

Source:http://linkedlifedata.com/resource/pubmed/id/7540207

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1995-7-18
pubmed:abstractText
The in vitro biological characterization of a series of 4-(alkylamino)-1,4-dihydroquinolines is reported. These compounds are novel inhibitors of voltage-activated n-type potassium ion (K+) channels in human T lymphocytes. This series, identified from random screening, was found to inhibit [125I]charybdotoxin binding to n-type K+ channels with IC50 values ranging from 10(-6) to 10(-8) M. These analogs also inhibit whole cell n-type K+ currents with IC50 values from 10(-5) to 10(-7) M. The preparation of a series of new 4-(alkylamino)-1,4-dihydroquinolines is described. Structure-activity relationships are discussed. Naphthyl analog 7c, the best compound prepared, exhibited > 100-fold selectivity for inhibition of [125I]charybdotoxin binding to n-type K+ channels compared with inhibition of [3H]dofetilide binding to cardiac K+ channels. These compounds represent a potent and selective series of n-type K+ channel inhibitors that have the potential for further development as anti-inflammatory agents.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
26
pubmed:volume
38
pubmed:owner
NLM
pubmed:authorsComplete
N
pubmed:pagination
1877-83
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Novel inhibitors of potassium ion channels on human T lymphocytes.
pubmed:affiliation
Sanofi Winthrop Inc., Collegeville, Pennsylvania 19426, USA.
pubmed:publicationType
Journal Article, Comparative Study