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Chloride channel blockers and activators act on anion channels that control cell volume, secretion and excitability. The main families are the chloride channel (ClC) family, calcium-activated chloride channels (CaCCs) and the cystic fibrosis transmembrane conductance regulator (CFTR). Expression cloning from the Torpedo electric organ in 1990 identified ClC-0, the first ClC channel. In 2008 three groups identified transmembrane protein 16A (TMEM16A, anoctamin 1) as a CaCC. T16Ainh-A01 and CaCCinh-A01 inhibit this conductance, and lubiprostone activates ClC-2 channels. Ivacaftor increases CFTR channel opening, whereas PPQ-102 blocks the CFTR channel. Chlorotoxin, a scorpion venom peptide, is used to study chloride currents and glioma cell binding.
Synonyms: Kalydeco; VX770
VX-770 (Ivacaftor) is known as a CFTR potentiator.
Adenophostin A is a potent modulator of inositol 1,4,5-trisphosphate receptors (IP3) that functions as a calcium (Ca2+) releaser, exhibiting an IC50 of 1.3 nM and an EC50 of 1.4 nM in rat models. This compound effectively stimulates Ca2+ release from intracellular stores and microsomes, inhibits the binding of [3H]IP3 to plasma membrane receptors, and activates chloride channels. Notably, Adenophostin A is resistant to phosphorylation and dephosphorylation by metabolic enzymes, thereby sustaining its activity and enhancing cytoplasmic Ca2+ levels in vascular smooth muscle cells. This reagent is highly relevant for research on hemorrhagic shock and related physiological studies.
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4''-Oxoavermectin B1a is a potent modulator of GABA (γ-aminobutyric acid) and glutamate-gated chloride channels, exhibiting significant insecticidal and acaricidal properties. This compound demonstrates efficacy in disrupting neurological processes in target pests, making it a valuable tool for research in agricultural pest management. Its application contributes to understanding the mechanisms of action in pest control strategies.
TMEM16A modulator-1 is a positive modulator of the calcium-activated chloride channel TMEM16A. This compound enhances the activity of TMEM16A, making it valuable for investigating its roles in various biological processes. It is particularly relevant for research into TMEM16A-related diseases, such as respiratory disorders, where modulation of ion channels may reveal therapeutic possibilities.
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