Potassium channel modulators
AssigneeMiles Inc.
InventorsRonald A. Janis, Frederick J. Hoffman, Jr.
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Abstract
An assay for detecting molecules and compounds which specifically bind to sites which regulate cellular potassium channels, for use, inter alia, as a method for identifying drugs with activity specific for modulating K.sup.+ channels.
Claims5
A method for identifying compounds capable of specific binding to K.sup.+ channels sensitive to tritiated (+)-N-(2-ethoxyphenyl)-N'-(1,2,2-trimethyl propyl)-2-nitroethene-1,1-diamine ([.sup.3 H]CMPD-I), said method comprising the following steps:
- (a) preparing a culture of a selected rat insulinoma (RIN) cell line;
- (b) adding [.sup.3 H]CMPD-I;
- (c) introducing a test compound;
- and
- (d) determining inhibition of specific binding of [.sup.3 H]CMPD-I by said test compound, wherein inhibition indicates the capacity of said test compound to specifically bind to said K.sup.+ channels sensitive to [.sup.3 H]CMPD-I.
A method for screening compounds capable of regulating K.sup.+ channels sensitive to tritiated (+)-N-(2-ethoxyphenyl)-N'-(1,2,2-trimethylpropyl)-2-nitroethene-1,1-diamin e ([.sup.3 H]CMPD-I), said method comprising the following steps:
- (a) preparing a selected rat insulinoma (RIN) cell line culture in an appropriate buffer and cell density;
- (b) replacing said buffer with a solution containing [.sup.3 H]CMPD-I;
- (c) adding a test compound at a selected concentration to form a mixture;
- (d) incubating said mixture at selected conditions;
- (e) separating bound [.sup.3 H]CMPD-I from free [.sup.3 H]CMPD-I in a suitable manner such as to form a counting sample;
- (f) counting said sample with a suitable detector for tritium;
- and
- (g) determining inhibition of specific binding of [.sup.3 H]CMPD-I by said test compound, wherein inhibition indicates the capacity of said test compound to regulate k.sup.+ channels sensitive to [.sup.3 H]CMPD-I.
Dependencies are inferred from the claim text.