Chloride channel blocker

A chloride channel blocker is a type of drug which inhibits the transmission of ions (Cl−) through chloride channels. Niflumic acid is a chloride channel blocker that has been used in experimental scientific research.[1] Another example is anthracene-9-carboxylic acid, a potent blocker of the CLCN1-type chloride channel found in skeletal muscle, which is used to study animal models of myotonia congenita.[2]

## See also

* Chloride channel opener

## References

1. ↑ Knauf, P. A. (1984). "Use of niflumic acid to determine the nature of the asymmetry of the human erythrocyte anion exchange system". The Journal of General Physiology 83 (5): 703–25. doi:10.1085/jgp.83.5.703. PMID 6736917.
2. ↑ Villegas-Navarro, A.; Martinez-Morales, M.; Morales-Aguilera, A. (1986). "Pharmacokinetics of anthracene-9-carboxylic acid, a potent myotonia-inducer". Archives Internationales de Pharmacodynamie et de Therapie 280 (1): 5–21. PMID 3718080.

## Further reading

* Phillis, J.W; Song, D.; O'Regan, M.H (1998). "Tamoxifen, a chloride channel blocker, reduces glutamate and aspartate release from the ischemic cerebral cortex". Brain Research 780 (2): 352–5. doi:10.1016/S0006-8993(97)01352-8. PMID 9507191.
* Zhou, Yuhong; Shapiro, Michael; Dong, Qu; Louahed, Jamila; Weiss, Christine; Wan, Shanhong; Chen, Qiming; Dragwa, Carl et al. (2008). "A Calcium-Activated Chloride Channel Blocker Inhibits Goblet Cell Metaplasia and Mucus Overproduction". Mucus Hypersecretion in Respiratory Disease. Novartis Foundation Symposia. pp. 150–170. doi:10.1002/0470860790.ch10. ISBN 9780470844786. https://books.google.com/books?id=yflNeSF5XygC&pg=PA150.
* Mohamed, Fahim; Senarathna, Lalith; Percy, Adrian; Abeyewardene, Manel; Eaglesham, Geoffrey; Cheng, Ron; Azher, Shifa; Hittarage, Ariyasena et al. (2004). "Acute Human Self‐Poisoning with theN‐Phenylpyrazole Insecticide Fipronil—a GABAA‐Gated Chloride Channel Blocker". Journal of Toxicology: Clinical Toxicology 42 (7): 955–63. doi:10.1081/CLT-200041784. PMID 15641641.
* Lukacs, Gergely L.; Nanda, Arvind; Rotstein, Ori D.; Grinstein, Sergio (1991). "The chloride channel blocker 5-nitro-2-(3-phenylpropyl-amino) benzoic acid (NPPB) uncouples mitochondria and increases the proton permeability of the plasma membrane in phagocytic cells". FEBS Letters 288 (1–2): 17–20. doi:10.1016/0014-5793(91)80992-C. PMID 1652470.
* Kang, J. X.; Man, S. F.; Brown, N. E.; Labrecque, P. A.; Clandinin, M. T. (1992). "The chloride channel blocker anthracene 9-carboxylate inhibits fatty acid incorporation into phospholipid in cultured human airway epithelial cells". Biochemical Journal 285 (3): 725–9. doi:10.1042/bj2850725. PMID 1323271.
* Liu, J.; Lai, Z. F.; Wang, X. D.; Tokutomi, N.; Nishi, K. (1998). "Inhibition of Sodium Current by Chloride Channel Blocker 4,4′-Diisothiocyanatostilbene-2,2′-Disulfonic Acid (DIDS) in Guinea Pig Cardiac Ventricular Cells". Journal of Cardiovascular Pharmacology 31 (4): 558–67. PMID 9554805. http://insights.ovid.com/pubmed?pmid=9554805.

* v
* t
* e

Pharmacomodulation

Types|

* ♦ Enzyme: Inducer
* Inhibitor

* ♦ Ion channel: Opener
* Blocker

* ♦ Receptor: Agonist
* Partial agonist
* Antagonist
* Inverse agonist
* Positive allosteric modulator (PAM)
* Negative allosteric modulator (NAM)

* ♦ Transporter [Reuptake vs Efflux]: Enhancer (RE)
* Inhibitor (RI)
* Releaser (RA)

* ♦ Miscellaneous: Precursor
* Cofactor

Classes|

| Enzyme|

see Enzyme inhibition

|

Ion channel|

See Ion channel modulators

Receptor &
transporter|

| BA/M|

| Adrenergic|

* Adrenergic receptor agonist (α
* β (1
* 2))
* Adrenergic receptor antagonist (α (1
* 2)
* β)
* Norepinephrine reuptake inhibitor (NRI)

|

Dopaminergic|

* Dopamine receptor agonist
* Dopamine receptor antagonist
* Dopamine reuptake inhibitor (DRI)

Histaminergic|

* Histamine receptor agonist
* Histamine receptor antagonist (H1
* H2
* H3)

Serotonergic|

* Serotonin receptor agonist
* Serotonin receptor antagonist (5-HT3)
* Serotonin reuptake inhibitor (SRI)

AA|

| GABAergic|

* GABA receptor agonist
* GABA receptor antagonist
* GABA reuptake inhibitor (GRI)

|

Glutamatergic|

* Glutamate receptor agonist (AMPA)
* Glutamate receptor antagonist (NMDA)
* Glutamate reuptake inhibitor

Cholinergic|

* Acetylcholine receptor agonist (Muscarinic
* Nicotinic)
* Acetylcholine receptor antagonist (Muscarinic
* Nicotinic (Ganglionic
* Muscular))

Cannabinoidergic|

* Cannabinoid receptor agonist
* Cannabinoid receptor antagonist
* Endocannabinoid enhancer (eCBE)
* Endocannabinoid reuptake inhibitor (eCBRI)

Opioidergic|

* Opioid modulator
* Opioid receptor agonist
* Opioid receptor antagonist
* Enkephalinase inhibitor

Other|

* Adenosine reuptake inhibitor (AdoRI)
* Angiotensin II receptor antagonist
* Endothelin receptor antagonist
* NK1 receptor antagonist
* Vasopressin receptor antagonist

Miscellaneous|

* Cofactor (see Enzyme cofactors)
* Precursor (see Amino acids)

* v
* t
* e

Ion channel modulators

Calcium|

| VDCCs|

| Blockers|

* L-type-selective: Dihydropyridines: Amlodipine
* Aranidipine
* Azelnidipine
* Barnidipine
* Clevidipine
* Cronidipine
* Darodipine
* Dexniguldipine
* Elgodipine
* Elnadipine
* Felodipine
* Flordipine
* Furnidipine
* Iganidipine
* Isradipine
* Lacidipine
* Lemildipine
* Lercanidipine
* Levamlodipine
* Levniguldipine
* Manidipine
* Mepirodipine
* Mesudipine
* Nicardipine
* Nifedipine
* Niguldipine
* Niludipine
* Nilvadipine
* Nimodipine
* Nisoldipine
* Nitrendipine
* Olradipine
* Oxodipine
* Palonidipine
* Pranidipine
* Ryodipine (riodipine)
* Sagandipine
* Sornidipine
* Teludipine
* Tiamdipine
* Trombodipine
* Vatanidipine; Diltiazem derivatives: Clentiazem
* Diltiazem
* Iprotiazem
* Nictiazem
* Siratiazem; Phenylalkylamines: Anipamil
* Dagapamil
* Devapamil
* Dexverapamil
* Emopamil
* Etripamil
* Falipamil
* Gallopamil
* Levemopamil
* Nexopamil
* Norverapamil
* Ronipamil
* Tiapamil
* Verapamil; Others: AH-1058
* Brinazarone
* Budiodarone
* Celivarone
* Cyproheptadine
* Dronedarone
* Fantofarone
* SR-33805
* Tetrahydropalmatine

* N-type-selective: ω-Conotoxins
* ω-Conotoxin GVIA
* Caroverine
* Huwentoxin XVI
* Leconotide (ω-conotoxin CVID)
* PD-173212
* Ralfinamide
* Safinamide
* Z160
* Ziconotide (ω-conotoxin MVIIA)

* P-type-selective: ω-Agatoxin IVA
* ω-Agatoxin IVB

* R-type-selective: SNX-482

* T-type-selective: ABT-639
* ML-218
* Niflumic acid
* NNC 55-0396
* ProTx I
* Z944
* Zonisamide

* Non-selective: ω-Agatoxin TK
* ω-Conotoxin MVIIC
* Benidipine
* Bepridil
* Cilnidipine
* Cinnarizine
* Dotarizine
* Efonidipine
* Flunarizine
* Lamotrigine
* Levetiracetam
* Lomerizine
* Loperamide
* Mibefradil
* NP078585
* Ruthenium red
* TROX-1

* α2δ subunit-selective (gabapentinoids): 4-Methylpregabalin
* Arbaclofen
* Arbaclofen placarbil
* Atagabalin
* Baclofen
* Gabapentin
* Gabapentin enacarbil
* Imagabalin
* Mirogabalin
* PD-200,347
* PD-217,014
* PD-299,685
* Phenibut
* Pregabalin

* Others/unsorted: Bencyclane
* Berbamine
* Bevantolol
* Canadine
* Carboxyamidotriazole
* Cycleanine
* Dauricine
* Dimeditiapramine
* Diproteverine
* Enpiperate
* Eperisone
* Elpetrigine
* Ethadione
* Ethanol (alcohol)
* Ethosuximide
* Fasudil
* Fendiline
* Fostedil
* Imepitoin
* JTV-519
* Lidoflazine
* Magnesium
* Manoalide
* Mesuximide
* Monatepil
* Naftopidil
* Ochratoxin A
* Osthol
* Otilonium bromide
* Paramethadione
* Phensuximide
* Pinaverium bromide
* Prenylamine
* Rhynchophylline
* Sesamodil
* Silperisone
* Sipatrigine
* Terodiline
* Tetrandrine
* Tolperisone
* Trimethadione
* Valperinol

|

Activators|

* L-type-selective: Bay K8644

Potassium|

| VGKCs|

| Blockers|

* 3,4-Diaminopyridine (amifampridine)
* 4-Aminopyridine (fampridine/dalfampridine)
* Adekalant
* Almokalant
* Amiodarone
* Azimilide
* Bretylium
* Bunaftine
* Charybdotoxin
* Clamikalant
* Conotoxins
* Dalazatide
* Dendrotoxin
* Dofetilide
* Dronedarone
* E-4031
* Hanatoxin
* HgeTx1
* HsTx1
* Ibutilide
* Inakalant
* Kaliotoxin
* Linopirdine
* Lolitrem B
* Maurotoxin
* Nifekalant
* Notoxin
* Paxilline
* Pinokalant
* Quinidine
* ShK-186
* Sotalol
* Tedisamil
* Terikalant
* Tetraethylammonium
* Vernakalant

* hERG (KCNH2, Kv11.1)-specific: Ajmaline
* Amiodarone
* AmmTX3
* Astemizole
* Azaspiracid
* AZD1305
* Azimilide
* Bedaquiline
* BeKm-1
* BmTx3
* BRL-32872
* Chlorpromazine
* Cisapride
* Clarithromycin
* Darifenacin
* Dextropropoxyphene
* Diallyl trisulfide
* Domperidone
* E-4031
* Ergtoxins
* Erythromycin
* Gigactonine
* Haloperidol
* Ketoconazole
* Norpropoxyphene
* Orphenadrine
* Pimozide
* PNU-282,987
* Promethazine
* Quinidine
* Ranolazine
* Roxithromycin
* Sertindole
* Solifenacin
* Tamulotoxin
* Terodiline
* Terfenadine
* Thioridazine
* Tolterodine
* Vanoxerine
* Vernakalant

* KCNQ (Kv7)-specific: Linopirdine
* XE-991
* Spooky toxin (SsTx)

|

Activators|

* KCNQ (Kv7)-specific: Flupirtine
* Retigabine

IRKs|

| Blockers|

* KATP-specific: Acetohexamide
* Carbutamide
* Chlorpropamide
* Glibenclamide (glyburide)
* Glibornuride
* Glicaramide
* Gliclazide
* Glimepiride
* Glipizide
* Gliquidone
* Glisoxepide
* Glyclopyramide
* Glycyclamide
* Metahexamide
* Mitiglinide
* Nateglinide
* Repaglinide
* Tolazamide
* Tolbutamide

* GIRK-specific: Barium
* Caramiphen
* Cloperastine
* Clozapine
* Dextromethorphan
* Ethosuximide
* Ifenprodil
* Tertiapin
* Tipepidine

|

Activators|

* KATP-specific: Aprikalim
* Bimakalim
* Cromakalim
* Diazoxide
* Emakalim
* Levcromakalim
* Mazokalim
* Minoxidil
* Naminidil
* Nicorandil
* Pinacidil
* Rilmakalim
* Sarakalim

* GIRK-specific: ML-297 (VU0456810)

KCa|

| Blockers|

* BKCa-specific: Ethanol (alcohol)
* GAL-021

|

Activators|

* BKCa-specific: Flufenamic acid
* Meclofenamic acid
* Niflumic acid
* Nimesulide
* Rottlerin (mallotoxin)
* Tolfenamic acid

K2Ps|

| Blockers|

* 12-O-Tetradecanoylphorbol-13-acetate
* Arachidonic acid
* Fluoxetine
* Norfluoxetine

|

Activators|

* Riluzole

Sodium|

| VGSCs|

| Blockers|

* Antianginals: Ranolazine

* Antiarrhythmics (class I): Ajmaline
* Aprindine
* Disopyramide
* Dronedarone
* Encainide
* Flecainide
* Lidocaine
* Lorajmine
* Lorcainide
* Mexiletine
* Moricizine
* Pilsicainide
* Prajmaline
* Procainamide
* Propafenone
* Quinidine
* Sparteine
* Tocainide

* Anticonvulsants: Acetylpheneturide
* Carbamazepine
* Cenobamate
* Chlorphenacemide
* Elpetrigine
* Eslicarbazepine acetate
* Ethotoin
* Fosphenytoin
* Lacosamide
* Licarbazepine
* Mephenytoin
* Oxcarbazepine
* Oxitriptyline
* Phenacemide
* Pheneturide
* Phenytoin
* Rufinamide
* Sipatrigine
* Topiramate
* Sodium valproate
* Valnoctamide
* Valproate pivoxil
* Valproate semisodium
* Valproic acid
* Valpromide
* Zonisamide

* Local anesthetics: pFBT
* Amylocaine
* Articaine
* Benzocaine
* Bupivacaine (Levobupivacaine, Ropivacaine)
* Butacaine
* Butamben
* Chloroprocaine
* Cinchocaine
* Cocaine
* Cyclomethycaine
* Dimethocaine
* Diphenhydramine
* Etidocaine
* Hexylcaine
* Iontocaine
* Lidocaine
* Mepivacaine
* Meprylcaine
* Metabutoxycaine
* Orthocaine
* Piperocaine
* Prilocaine
* Procaine
* Propoxycaine
* Proxymetacaine
* Risocaine
* Tetracaine
* Trimecaine

* Analgesics: AZD-3161
* DSP-2230
* Funapide
* GDC-0276
* NKTR-171
* PF-04531083
* PF-05089771
* Ralfinamide
* Raxatrigine
* RG7893 (GDC-0287)

* Toxins: Conotoxins
* Neosaxitoxin
* Saxitoxin
* Tetrodotoxin
* Zetekitoxin AB

* Others: Buprenorphine
* Evenamide
* Menthol (mint)
* Safinamide
* Tricyclic antidepressants

|

Activators|

* Aconitine
* Atracotoxins (ω-Atracotoxin, Robustoxin, Versutoxin)
* Batrachotoxin
* Ciguatoxins
* Grayanotoxins
* Poneratoxin

ENaC|

| Blockers|

* Amiloride
* Benzamil
* Triamterene

|

Activators|

* Solnatide

ASICs|

| Blockers|

* A-317567
* Amiloride
* Aspirin
* Ibuprofen
* PcTX1

|

Chloride|

| CaCCs|

| Blockers|

* Crofelemer
* DIDS
* Ethacrynic acid
* Flufenamic acid
* Fluoxetine
* Furosemide
* Glibenclamide
* Mefloquine
* Mibefradil
* Niflumic acid

|

Activators|

* Carbachol

CFTR|

| Blockers|

* Glibenclamide
* Lonidamine
* Piretanide

|

Activators|

* 1,7-Phenanthroline
* 1,10-Phenanthroline
* 4,7-Phenanthroline
* 7,8-Benzoquinoline
* Ivacaftor
* Phenanthridine

Unsorted|

| Blockers|

* Bumetanide
* Flufenamic acid
* Meclofenamic acid
* Mefenamic acid
* Mepacrine
* Niflumic acid
* Talniflumate
* Tolfenamic acid
* Trifluoperazine

|

Others|

| TRPs|

* See here instead.

|

LGICs|

* See here instead.

See also: Receptor/signaling modulators • Transient receptor potential channel modulators

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*[v]: View this template
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*[VDCCs]: Voltage-dependent calcium channels
*[VGKCs]: Voltage-gated potassium channels
*[IRKs]: Inwardly rectifying potassium channel
*[KATP]: ATP-sensitive potassium channel
*[GIRK]: G protein-coupled inwardly-rectifying potassium channel
*[KCa]: Calcium-activated potassium channel
*[K2Ps]: Tandem pore domain potassium channel
*[VGSCs]: Voltage-gated sodium channels
*[ENaC]: Epithelial sodium channel
*[ASICs]: Acid-sensing ion channel
*[CaCCs]: Calcium-activated chloride channel
*[CFTR]: Cystic fibrosis transmembrane conductance regulator
*[TRPs]: Transient receptor potential channels
*[LGICs]: Ligand gated ion channels