Chloride channel

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.

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.

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.

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.

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.

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.

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).

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.

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.

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.

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

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

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.

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.

MONNA is a potent TMEM16A (Anoctamin-1) blocker (IC50 : 80 nM). It induces vasorelaxation of rodent resistance arteries in presence or absence of chloride ions.

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.

Ani9 is a high selective blocker of Anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A) with an IC50 of 77 nM and can be used in studies about ANO1 and the treatment of ancer, hypertension, pain, diarrhea and asthma.

R(+)-IAA-94 (R(+)-Methylindazone) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-IAA-94 inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).

NS1652 is an anion conductance inhibitor. NS1652 blocks chloride channel has an IC50 of 1.6 μM in human and mouse red blood cells.

Picrotin is an inhibitor of glycine receptors. Picrotin blocks α2 GlyR, α1 GlyR, and α3 GlyR and can be used in studies about neurotransmission.

Adjudin (AF-2364) is a small molecule compound known to possess antispermatogenic function, attenuates microglia activation by suppression of the NF-κB pathway.

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.

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

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.

Isodeoxycholic Acid is a bile acid that is formed via epimerization of deoxycholic acid by intestinal bacteria. It has a greater critical micelle concentration than DCA, indicating reduced detergent activity, and is less active than DCA in inhibiting growth in a panel of seven gut commensal bacteria species. Isodeoxycholic Acid(0.1%) inhibits spore germination induced by taurocholic acid in several C. difficile strains, as well as decreases the cytotoxicity of C. difficile culture supernatants to Vero cells. Plasma levels of isodeoxycholic acid are decreased in a rat model of high-fat diet-induced obesity compared with rats fed a normal diet.

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

Eact is a selective and potent TMEM16A activator. It directly activates the TRPV1 channels in sensory nociceptors. Which also produces itch, acute nociception and thermal hypersensitivity.

Endovion (NS3728) is a pharmacological anion channel and an Anoctamin-1 (ANO 1) channel inhibitor. Endovion is also the specific VRAC/VSOAC blocker.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.

CaCCinh-A01 is an inhibitor of the calcium-activated chloride channel (CaCC, 10 μM) and TMEM16A (IC50: 2.1 μM).