The antiparasitic drug ivermectin (shown here in royal blue) works by binding to glutamate-gated chloride channel receptors, a type of chloride channel found only in protostomes. It “locks” the receptor in an activated (open) conformation, allowing unrestricted passage of chloride (Cl−) ions into the cell, ultimately killing the parasite. (Top view shows the open channel, with a central pore through which Cl− is transported; side view shows drug binding. From PDB: 3RHW.)
A chloride channel opener is a type of drug which facilitates ion transmission through chloride channels.
An example is 1,10-phenanthroline, which activates Cystic fibrosis transmembrane conductance regulator (CFTR) chloride channels.
GABA-A receptor agonists (e.g. lorazepam) may also be considered chloride channel openers
See also
Further reading
- Cuthbert AW (February 2001). "Assessment of CFTR chloride channel openers in intact normal and cystic fibrosis murine epithelia". British Journal of Pharmacology. 132 (3): 659–68. doi:10.1038/sj.bjp.0703859. PMC 1572602. PMID 11159718.
- Ramteke VD, Tandan SK, Kumar D, Aruna Devi R, Shukla MK, Ravi Prakash V (January 2009). "Increased hyperalgesia by 5-nitro-2, 3-(phenylpropylamino)-benzoic acid (NPPB), a chloride channel blocker in crush injury-induced neuropathic pain in rats". Pharmacology Biochemistry and Behavior. 91 (3): 417–22. doi:10.1016/j.pbb.2008.08.017. PMID 18775743. S2CID 20051233.