Chloride channel opener

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

References[]

^ 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.
^ 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[]

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.

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[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.

[pmid11606326-2] 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.

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[2]

Chloride channel opener

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