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.[1] (Top view shows the open channel, with a central pore through which Cl− is transported; side view shows drug binding. From PDB: 3RHW​.)
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.[1] (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.[2]

GABA-A receptor agonists (e.g. lorazepam) may also be considered chloride channel openers

See also

References

  1. ^ Atif M, Estrada-Mondragon A, Nguyen B, Lynch JW, Keramidas A (October 2017). "Effects of glutamate and ivermectin on single glutamate-gated chloride channels of the parasitic nematode H. contortus". PLOS Pathog. 13 (10): e1006663. doi:10.1371/journal.ppat.1006663. PMC 5638611. PMID 28968469.
  2. ^ Duszyk M, MacVinish L, Cuthbert AW (October 2001). "Phenanthrolines--a new class of CFTR chloride channel openers". British Journal of Pharmacology. 134 (4): 853–64. doi:10.1038/sj.bjp.0704328. PMC 1573018. PMID 11606326.

Further reading