Chloride channel openers refer to a specific category of drugs designed to modulate chloride channels in the human body. Chloride channels are anion-selective channels which are involved in a wide variety of physiological functions and processes such as the regulation of neuroexcitation, transepithelial salt transport, and smooth muscle contraction.[1] Due to their distribution throughout the body, diversity, functionality, and associated pathology, chloride channels[2] represent an ideal target for the development of channel modulating drugs such as chloride channel openers.
Chloride channel modulators include chloride channel openers, and chloride channel blockers, both of which modulate the transport of chloride ions through chloride channels.[3] Chloride channel openers specifically work by either preventing the closure of chloride channels, or promoting their opening, thus helping to facilitate movement of chloride ions into a cell.
In general, mutations in various chloride channels throughout the human body can result in many pathologies, such as macular degeneration, myotonia, cystic fibrosis, and hyperekplexia.[3]
Chloride channel openers have been proposed to treat a variety of such pathologies, most notably including cystic fibrosis, a genetic disorder in which a defect in the cystic fibrosis transmembrane conductance regulator protein impacts chloride ion transport across epithelial cells.[4]
Chloride channels remain a somewhat under-explored target for drug development despite their biological significance, due to various issues associated with the development of successful chloride channel drugs. As a result, the development of chloride channel modulators such as chloride channel opening drugs has been limited. The relative structural complexity of chloride channels, their varied roles in biological processes, and the problems associated with the development of drugs with high specificity emphasize the necessity for further research in this area.
^"Chloride Channels". British Journal of Pharmacology. 158 (Suppl 1): 130–134. November 2009. doi:10.1111/j.1476-5381.2009.00503_6.x (inactive 2024-03-22). PMC 2884561.{{cite journal}}: CS1 maint: DOI inactive as of March 2024 (link)
Chloridechannelopeners refer to a specific category of drugs designed to modulate chloridechannels in the human body. Chloridechannels are anion-selective...
channelopener Sodium channel: see also Sodium channel blocker, Sodium channelopenerChloridechannel: see also Chloridechannel blocker, Chloride channel...
glycine receptors and GABAA receptors also act as chloridechannel blockers. Chloridechannelopener Knauf PA, Mann NA (May 1984). "Use of niflumic acid...
A potassium channelopener is a type of drug which facilitates ion transmission through potassium channels. Some examples include: Diazoxide vasodilator...
specific ion channels. These are classified by the channel on which they act: Calcium channelopeners, such as Bay K8644 Chloridechannelopeners, such as...
even death, as might be expected from potentiation of inhibitory chloridechannels. Since drugs that inhibit the enzyme CYP3A4 often also inhibit P-glycoprotein...
A sodium channelopener is a type of drug which facilitates ion transmission through sodium channels. Examples include toxins, such as aconitine, veratridine...
transport chloride through the channel. Ivacaftor, a CFTR potentiator, improves the transport of chloride through the ion channel by binding to the channels directly...
A calcium channelopener is a type of drug which facilitates ion transmission through calcium channels. An example is Bay K8644, which is an analogue of...
voltage-gated sodium channels, such as CNV1014802 and Funapide, are being investigated as novel analgesics. Sodium channelopener Sodium+Channel+Blockers at the...
medication that has the dual properties of a nitrate and ATP-sensitive K+ channelopener. In humans, the nitrate action of nicorandil dilates the large coronary...
Dihydropyridine calcium channel blockers are derivatives of 1,4-dihydropyridine that are used as L-type calcium channel blockers. They are used in the...
conductance potassium channel (BKCa++) opener. BKCa++ is found in the inner mitochondrial membrane of cardiomyocytes. Opening these channels is beneficial for...
potassium channelopener, causing hyperpolarization of cell membranes. Theoretically, by widening blood vessels and opening potassium channels, it allows...
"Noble gas xenon is a novel adenosine triphosphate-sensitive potassium channelopener". Anesthesiology. 112 (3): 623–30. doi:10.1097/ALN.0b013e3181cf894a...
propylamino-benzoic acid) was shown, in the same study, to be a more effective chloridechannel blocker. Finally it may act by inhibiting calcium influx. Cromoglicate...
release through its action on potassium channels. Diazoxide is one of the most potent openers of the K+ ATP channels present on the insulin producing beta...
(INN) is a potassium channel-opening vasodilator. The active isomer is levcromakalim. It acts on ATP-sensitive potassium channels and so causes membrane...
pharmacological modulators of potassium channels, see potassium channel blocker and potassium channelopener. Potassium channels have a tetrameric structure in...
a toxin which acts as a large conductance Ca2+-activated K+ channel (BK channel) opener. IPA originates from many sorts of trees, especially conifers...
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