chloride channel

Niflumic acid (Nifluril) is a Ca2+-activated Cl- channel blocker and an analgesic and anti-inflammatory agent used in the therapy of rheumatoid arthritis.

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.

ANO1-IN-1, a selective ANO1 channel blocker, inhibited ANO1 and ANO2 with IC50 values of 2.56 μM and 15.43 μM, respectively.ANO1-IN-1 had a significant inhibitory effect on the proliferation of glioma cells.

ANO1-IN-4 (Compound 10bm) is a reversible inhibitor of the calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1), with an IC50 of 0.030 µM. It demonstrates good metabolic stability in rat liver microsomes and can inhibit spontaneous contractions in isolated mouse ileum.

Crofelemer (Provir) is an orally active antidiarrheal agent. It targets the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CACC), which are responsible for chloride and fluid secretion in the gastrointestinal tract. Crofelemer is applicable for research in diarrhea-related conditions.

S9-A13 is a potent and selective inhibitor of SLC26A9, exhibiting an IC50 of 90.9 nM without inhibiting other members of the SLC26 family, such as SLC26A3, SLC26A4, and SLC26A6. It also inhibits the SLC26A9 Cl- current in cells lacking CFTR expression.

Fenamic acid (N-Phenylanthranilic acid) is a chloride channel blocker that causes renal papillary necrosis in rats. Fenamic acid serves as a parent structure for several nonsteroidal anti-inflammatory drugs (NSAIDs), including flufenamic acid, tolfenamic acid, mefenamic acid, and meclofenamic acid.

Selamectin (UK-124114) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg ml) shows the effect of growth inhibition.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

Meticrane (Arresten) is a sulphonamide-derivative with thiazide-like diuretic activity.

Alanine is a nonessential amino acid made in the body from the conversion of the carbohydrate pyruvate or the breakdown of DNA and the dipeptides carnosine and anserine. D-Alanine ((R)-Alanine) is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.

Betaine chloride (Betaine hydrochloride) is an acidic form of betaine, a vitamin-like substance observed in grains and other foods; gains the amplification of DNA by decreasing the formation of secondary structure in GC-rich regions.

Picrotoxinin is a blocker of chloride channel and a noncompetitive antagonist of GABAA with an IC50 of 1.15 μM for α1β2γ2L GABAA. Picrotoxinin shows convulsant properties.

T16Ainh-A01 is a potent inhibitor of TMEM16A Chloride channel, inhibiting TMEM16A-mediated chloride currents (IC50 of 1 µM),and functions as a calcium-activated chloride channel (CaCC).

Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.

Talniflumate (Somalgen) is a calcium-activated chloride channel (hCLCA1 mCLCA3) blocker that reduces mucin synthesis and releases in animal models and cell culture. It possesses anti-inflammatory actions via inhibition of Cox (cyclooxygenase) and inhibits Cl- HCO3- exchange activity. It also increases survival in a cystic fibrosis mouse model of the distal intestinal obstructive syndrome.

Lubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation.

Afoxolaner is an isoxazoline insecticide acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

NPPB is a chloride channel blocker with IC50 of 80 nM .

Irisolidone is a potent volume-regulated anion channel (VRAC) current inhibitor, it exhibits high efficacy for VRAC blockade with IC50s of 5-13 μM.

Guanidinoethyl sulfonate (Taurocyamine) is a competitive glycine receptor antagonist.

Hypotaurine (2-Aminoethanesulfinic acid), functioning as an intermediate in the biosynthesis of taurine from cysteine within astrocytes, acts as an endogenous inhibitory amino acid targeting the glycine receptor.