Article
Novel nonpeptide agents potently block the C-type inactivated conformation of Kv1.3 and suppress T cell activation.
Molecular pharmacology - 1 Dec 1996
Nguyen A, Kath J C, Hanson D C, Biggers M S, Canniff P C, Donovan C B, Mather R J, Bruns M J, Rauer H, Aiyar J, Lepple-Wienhues A, Gutman G A, Grissmer S, Cahalan M D, Chandy K G
Abstract excerpt
The nonpeptide agent CP-339,818 (1-benzyl-4-pentylimino-1,4-dihydroquinoline) and two analogs (CP-393,223 and CP-394,322) that differ only with respect to the type of substituent at the N1 position, potently blocked the Kv1.3 channel in T lymphocytes. A fourth compound (CP-393,224), which has a smaller and less-lipophilic group at N1, was 100-200-fold less potent, suggesting that a large lipophilic group at this...
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