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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.
W F Michne, and
J W Guiles, and
A M Treasurywala, and
L A Castonguay, and
C A Weigelt, and
B Oconnor, and
W A Volberg, and
A M Grant, and
C C Chadwick, and
D S Krafte
April 1989,
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W F Michne, and
J W Guiles, and
A M Treasurywala, and
L A Castonguay, and
C A Weigelt, and
B Oconnor, and
W A Volberg, and
A M Grant, and
C C Chadwick, and
D S Krafte
January 1992,
The Journal of physiology,
W F Michne, and
J W Guiles, and
A M Treasurywala, and
L A Castonguay, and
C A Weigelt, and
B Oconnor, and
W A Volberg, and
A M Grant, and
C C Chadwick, and
D S Krafte
January 1987,
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W F Michne, and
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A M Treasurywala, and
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W A Volberg, and
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May 1997,
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W F Michne, and
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A M Treasurywala, and
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D S Krafte
June 2005,
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W F Michne, and
J W Guiles, and
A M Treasurywala, and
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A M Grant, and
C C Chadwick, and
D S Krafte
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C A Weigelt, and
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A M Grant, and
C C Chadwick, and
D S Krafte
October 1994,
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W F Michne, and
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A M Treasurywala, and
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C A Weigelt, and
B Oconnor, and
W A Volberg, and
A M Grant, and
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D S Krafte
March 1990,
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W F Michne, and
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A M Treasurywala, and
L A Castonguay, and
C A Weigelt, and
B Oconnor, and
W A Volberg, and
A M Grant, and
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D S Krafte
May 2005,
The Journal of membrane biology,
W F Michne, and
J W Guiles, and
A M Treasurywala, and
L A Castonguay, and
C A Weigelt, and
B Oconnor, and
W A Volberg, and
A M Grant, and
C C Chadwick, and
D S Krafte
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