Page last updated: 2024-10-24

chloride channel inhibitor activity

Definition

Target type: molecularfunction

Binds to and stops, prevents, or reduces the activity of a chloride channel. [GOC:mah]

Chloride channel inhibitor activity refers to the ability of a molecule to block or reduce the flow of chloride ions (Cl-) through chloride channels. Chloride channels are transmembrane proteins that form pores in cell membranes, allowing the passage of chloride ions. These channels play crucial roles in various physiological processes, including:

- **Cell volume regulation:** Chloride channels contribute to the maintenance of cell volume by regulating the movement of chloride ions in and out of the cell.
- **Nerve impulse transmission:** Chloride channels are involved in the propagation of nerve impulses by modulating the electrical potential across neuronal membranes.
- **Muscle contraction:** Chloride channels influence muscle contraction by controlling the flow of chloride ions into muscle cells.
- **Epithelial transport:** Chloride channels facilitate the transport of chloride ions across epithelial tissues, contributing to processes like fluid secretion and absorption.
- **pH regulation:** Chloride channels play a role in pH regulation by mediating the movement of bicarbonate ions, which are involved in acid-base balance.

Chloride channel inhibitors can act by different mechanisms:

- **Binding to the channel pore:** Some inhibitors directly bind to the pore of the chloride channel, physically blocking the passage of chloride ions.
- **Altering channel conformation:** Other inhibitors bind to sites outside the pore, inducing conformational changes in the channel protein that hinder chloride ion flow.
- **Modulating channel gating:** Some inhibitors affect the opening and closing of chloride channels, reducing their overall activity.

The specific molecular mechanisms of chloride channel inhibitor activity can vary depending on the type of channel, the inhibitor molecule, and the physiological context. However, the common denominator is the disruption of chloride ion flow through chloride channels, leading to a variety of cellular and physiological effects.

Understanding chloride channel inhibitor activity is crucial for developing drugs that target chloride channels for therapeutic purposes. For example, chloride channel inhibitors are being investigated for their potential in treating diseases such as cystic fibrosis, epilepsy, and cancer.'
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Proteins (1)

ProteinDefinitionTaxonomy
Cystic fibrosis transmembrane conductance regulatorA cystic fibrosis transmembrane conductance regulator that is encoded in the genome of human. [PRO:CNA, UniProtKB:P13569]Homo sapiens (human)

Compounds (13)

CompoundDefinitionClassesRoles
glyburideglyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.

Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide
monochlorobenzenes;
N-sulfonylurea
anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
methyl anthranilatemethyl anthranilate : A benzoate ester that is the methyl ester of anthranilic acid.benzoate esterflavouring agent;
metabolite
telmisartantelmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.

Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.
benzimidazoles;
biphenyls;
carboxybiphenyl
angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
tadalafilbenzodioxoles;
pyrazinopyridoindole
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine
3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone: a cystic fibrosis transmembrane conductance regulator inhibitor; structure in first source
uccf-029organic heterotricyclic compound;
organooxygen compound
quercetin7-hydroxyflavonol;
pentahydroxyflavone
antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
apigeninChamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.trihydroxyflavoneantineoplastic agent;
metabolite
rutinHydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders.disaccharide derivative;
quercetin O-glucoside;
rutinoside;
tetrahydroxyflavone
antioxidant;
metabolite
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
vx-770ivacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis.

ivacaftor: a CFTR potentiator; structure in first source
aromatic amide;
monocarboxylic acid amide;
phenols;
quinolone
CFTR potentiator;
orphan drug
lumacaftorlumacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropane-1-carboxylic acid with the aromatic amino group of 3-(6-amino-3-methylpyridin-2-yl)benzoic acid. Used for the treatment of cystic fibrosis.

lumacaftor: a corrector of CF transmembrane conductance regulator (CTFR); structure in first source
aromatic amide;
benzodioxoles;
benzoic acids;
cyclopropanes;
organofluorine compound;
pyridines
CFTR potentiator;
orphan drug