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
References
- ↑ 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.
- ↑ 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.
Pharmacomodulation |
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| 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
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| Classes | | Enzyme | see Enzyme inhibition |
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| Ion channel | See Ion channel modulators |
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Receptor & transporter | | BA/M | | Adrenergic |
- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2)
- β)
- Norepinephrine reuptake inhibitor (NRI)
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| Dopaminergic |
- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
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| Histaminergic |
- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
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| Serotonergic |
- Serotonin receptor agonist
- Serotonin receptor antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
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| AA | | GABAergic |
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
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| Glutamatergic |
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
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| Cholinergic |
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
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| Cannabinoidergic |
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
- Endocannabinoid enhancer (eCBE)
- Endocannabinoid reuptake inhibitor (eCBRI)
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| Opioidergic |
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
- Enkephalinase inhibitor
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| Other |
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
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| Miscellaneous |
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
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Ion channel modulators |
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| Calcium | | VDCCs | | Blockers | |
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| Activators |
- L-type-selective: Bay K8644
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| Potassium | |
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| Sodium | |
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| Chloride | | CaCCs | | Blockers |
- Crofelemer
- DIDS
- Ethacrynic acid
- Flufenamic acid
- Fluoxetine
- Furosemide
- Glibenclamide
- Mefloquine
- Mibefradil
- Niflumic acid
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| Activators | |
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| CFTR | | Blockers |
- Glibenclamide
- Lonidamine
- Piretanide
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| Activators |
- 1,7-Phenanthroline
- 1,10-Phenanthroline
- 4,7-Phenanthroline
- 7,8-Benzoquinoline
- Ivacaftor
- Phenanthridine
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| Unsorted | | Blockers |
- Bumetanide
- Flufenamic acid
- Meclofenamic acid
- Mefenamic acid
- Mepacrine
- Niflumic acid
- Talniflumate
- Tolfenamic acid
- Trifluoperazine
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| Others | |
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See also: Receptor/signaling modulators • Transient receptor potential channel modulators |