Chloride channel blocker explained

A chloride channel blocker is a type of drug which inhibits the transmission of ions (Cl⁻) through chloride channels.

Niflumic acid is a chloride channel blocker that has been used in experimental scientific research.^[1] Another example is anthracene-9-carboxylic acid, a potent blocker of the CLCN1-type chloride channel found in skeletal muscle, which is used to study animal models of myotonia congenita.^[2]

Some antagonists of glycine receptors and GABAA receptors also act as chloride channel blockers.

See also

• Chloride channel opener

Further reading

• Phillis JW, Song D, O'Regan MH . Tamoxifen, a chloride channel blocker, reduces glutamate and aspartate release from the ischemic cerebral cortex . Brain Research . 780 . 2 . 352–5 . January 1998 . 9507191 . 10.1016/S0006-8993(97)01352-8 . 3160962 .
• Book: 10.1002/0470860790.ch10 . . Mucus Hypersecretion in Respiratory Disease . 150–170 . Novartis Foundation Symposia . Zhou . Yuhong . Shapiro . Michael . Dong . Qu . Louahed . Jamila . Weiss . Christine . Wan . Shanhong . Chen . Qiming . Dragwa . Carl . Savio . Dawn . Huang . Minxue . Fuller . Catherine . Tomer . Yaniv . Nicolaides . Nicholas C. . McLane . Michael . Levitt . Roy C. . A Calcium-Activated Chloride Channel Blocker Inhibits Goblet Cell Metaplasia and Mucus Overproduction . 2002 . 248 . 9780470844786 .
• Mohamed F, Senarathna L, Percy A, Abeyewardene M, Eaglesham G, Cheng R, Azher S, Hittarage A, Dissanayake W, Sheriff MH, Davies W, Buckley NA, Eddleston M . Acute human self-poisoning with the N-phenylpyrazole insecticide fipronil--a GABAA-gated chloride channel blocker . Journal of Toxicology. Clinical Toxicology . 42 . 7 . 955–63 . 2004 . 15641641 . 1351141 . 10.1081/CLT-200041784 .
• Lukacs GL, Nanda A, Rotstein OD, Grinstein S . The chloride channel blocker 5-nitro-2-(3-phenylpropyl-amino) benzoic acid (NPPB) uncouples mitochondria and increases the proton permeability of the plasma membrane in phagocytic cells . FEBS Letters . 288 . 1–2 . 17–20 . August 1991 . 1652470 . 10.1016/0014-5793(91)80992-C . 35959479 . free .
• Kang JX, Man SF, Brown NE, Labrecque PA, Clandinin MT . The chloride channel blocker anthracene 9-carboxylate inhibits fatty acid incorporation into phospholipid in cultured human airway epithelial cells . The Biochemical Journal . 285 (Pt 3) . 3 . 725–9 . August 1992 . 1323271 . 1132855 . 10.1042/bj2850725 .
• Liu J, Lai ZF, Wang XD, Tokutomi N, Nishi K . Inhibition of sodium current by chloride channel blocker 4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS) in guinea pig cardiac ventricular cells . Journal of Cardiovascular Pharmacology . 31 . 4 . 558–67 . April 1998 . 9554805 . 10.1097/00005344-199804000-00014 . free .

Notes and References

1. Knauf PA, Mann NA . Use of niflumic acid to determine the nature of the asymmetry of the human erythrocyte anion exchange system . The Journal of General Physiology . 83 . 5 . 703–25 . May 1984 . 6736917 . 2215658 . 10.1085/jgp.83.5.703 .
2. Villegas-Navarro A, Martinez-Morales M, Morales-Aguilera A . Pharmacokinetics of anthracene-9-carboxylic acid, a potent myotonia-inducer . Archives Internationales de Pharmacodynamie et de Thérapie . 280 . 1 . 5–21 . March 1986 . 3718080 .