{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,28]],"date-time":"2026-09-28T22:05:34Z","timestamp":1790633134325,"version":"4.1.0"},"reference-count":39,"publisher":"Elsevier BV","issue":"1","license":[{"start":{"date-parts":[[2009,7,1]],"date-time":"2009-07-01T00:00:00Z","timestamp":1246406400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2009,7,1]],"date-time":"2009-07-01T00:00:00Z","timestamp":1246406400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"content-domain":{"domain":["molpharm.aspetjournals.org","elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Molecular Pharmacology"],"published-print":{"date-parts":[[2009,7]]},"DOI":"10.1124\/mol.108.053744","type":"journal-article","created":{"date-parts":[[2009,4,30]],"date-time":"2009-04-30T00:54:26Z","timestamp":1241052866000},"page":"105-112","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":146,"title":["Inhibition of Aquaporin-1 and Aquaporin-4 Water Permeability by a Derivative of the Loop Diuretic Bumetanide Acting at an Internal Pore-Occluding Binding Site"],"prefix":"10.1016","volume":"76","author":[{"given":"Elton","family":"Migliati","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nathalie","family":"Meurice","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Pascale","family":"DuBois","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jennifer S.","family":"Fang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Suma","family":"Somasekharan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elizabeth","family":"Beckett","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gary","family":"Flynn","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andrea J.","family":"Yool","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1124\/mol.108.053744_bib1","doi-asserted-by":"crossref","unstructured":"Agre P, Preston GM, Smith BL, Jung JS, Raina S, Moon C, Guggino WB, and Nielsen S (1993) Aquaporin CHIP: the archetypal molecular water channel. Am J Physiol 265: F463-F476.","DOI":"10.1152\/ajprenal.1993.265.4.F463"},{"key":"10.1124\/mol.108.053744_bib2","doi-asserted-by":"crossref","unstructured":"Amiry-Moghaddam M, Frydenlund DS, and Ottersen OP (2004a) Anchoring of aquaporin-4 in brain: molecular mechanisms and implications for the physiology and pathophysiology of water transport. Neuroscience 129: 999-1010.","DOI":"10.1016\/j.neuroscience.2004.08.049"},{"key":"10.1124\/mol.108.053744_bib3","doi-asserted-by":"crossref","unstructured":"Amiry-Moghaddam M, Xue R, Haug FM, Neely JD, Bhardwaj A, Agre P, Adams ME, Froehner SC, Mori S, and Ottersen OP (2004b) Alpha-syntrophin deletion removes the perivascular but not endothelial pool of aquaporin-4 at the blood-brain barrier and delays the development of brain edema in an experimental model of acute hyponatremia. FASEB J 18: 542-544.","DOI":"10.1096\/fj.03-0869fje"},{"key":"10.1124\/mol.108.053744_bib4","doi-asserted-by":"crossref","unstructured":"Boassa D and Yool AJ (2002) A fascinating tail: cGMP activation of aquaporin-1 ion channels. Trends Pharmacol Sci 23: 558-562.","DOI":"10.1016\/S0165-6147(02)02112-0"},{"key":"10.1124\/mol.108.053744_bib5","doi-asserted-by":"crossref","unstructured":"Boassa D and Yool AJ (2003) Single amino acids in the carboxyl terminal domain of aquaporin-1 contribute to cGMP-dependent ion channel activation. BMC Physiol 3: 12.","DOI":"10.1186\/1472-6793-3-12"},{"key":"10.1124\/mol.108.053744_bib6","doi-asserted-by":"crossref","unstructured":"Brooks HL, Regan JW, and Yool AJ (2000) Inhibition of aquaporin-1 water permeability by tetraethylammonium: involvement of the loop E pore region. Mol Pharmacol 57: 1021-1026.","DOI":"10.1016\/S0026-895X(24)26513-5"},{"key":"10.1124\/mol.108.053744_bib7","doi-asserted-by":"crossref","unstructured":"Cooper GJ and Boron WF (1998) Effect of PCMBS on CO2 permeability of Xenopus oocytes expressing aquaporin 1 or its C189S mutant. Am J Physiol 275: C1481-C1486.","DOI":"10.1152\/ajpcell.1998.275.6.C1481"},{"key":"10.1124\/mol.108.053744_bib8","doi-asserted-by":"crossref","unstructured":"Darman RB and Forbush B (2002) A regulatory locus of phosphorylation in the N terminus of the Na-K-Cl cotransporter, NKCC1. J Biol Chem 277: 37542-37550.","DOI":"10.1074\/jbc.M206293200"},{"key":"10.1124\/mol.108.053744_bib9","doi-asserted-by":"crossref","unstructured":"Detmers FJ, de Groot BL, M\u00fcller EM, Hinton A, Konings IB, Sze M, Flitsch SL, Grubm\u00fcller H, and Deen PM (2006) Quaternary ammonium compounds as water channel blockers. Specificity, potency, and site of action. J Biol Chem 281: 14207-14214.","DOI":"10.1074\/jbc.M513072200"},{"key":"10.1124\/mol.108.053744_bib10","doi-asserted-by":"crossref","unstructured":"Edelsbrunner H, Facello M, Fu R, and Liang J (1995) Measuring proteins and voids in proteins, in Proceedings of the 28th Annual Hawaii International Conference on System Sciences (HICSS-28); 1995 Jan 3-6; Kihei, Maui, Hawaii; pp 256-264, IEEE Computer Society, Washington, DC.","DOI":"10.1109\/HICSS.1995.375331"},{"key":"10.1124\/mol.108.053744_bib11","doi-asserted-by":"crossref","unstructured":"Fotiadis D, Suda K, Tittmann P, Jen\u00f6 P, Philippsen A, M\u00fcller DJ, Gross H, and Engel A (2002) Identification and structure of a putative Ca2+-binding domain at the C terminus of AQP1. J Mol Biol 318: 1381-1394.","DOI":"10.1016\/S0022-2836(02)00143-2"},{"key":"10.1124\/mol.108.053744_bib12","doi-asserted-by":"crossref","unstructured":"Frigeri A, Nicchia GP, Nico B, Quondamatteo F, Herken R, Roncali L, and Svelto M (2001) Aquaporin-4 deficiency in skeletal muscle and brain of dystrophic mdx mice. FASEB J 15: 90-98.","DOI":"10.1096\/fj.00-0260com"},{"key":"10.1124\/mol.108.053744_bib13","doi-asserted-by":"crossref","unstructured":"Hiroaki Y, Tani K, Kamegawa A, Gyobu N, Nishikawa K, Suzuki H, Walz T, Sasaki S, Mitsuoka K, Kimura K, et al. (2006) Implications of the aquaporin-4 structure on array formation and cell adhesion. J Mol Biol 355: 628-639.","DOI":"10.1016\/j.jmb.2005.10.081"},{"key":"10.1124\/mol.108.053744_bib14","doi-asserted-by":"crossref","unstructured":"Hohmann I, Bill RM, Kayingo I, and Prior BA (2000) Microbial MIP channels. Trends Microbiol 8: 33-38.","DOI":"10.1016\/S0966-842X(99)01645-5"},{"key":"10.1124\/mol.108.053744_bib15","doi-asserted-by":"crossref","unstructured":"Huber VJ, Tsujita M, Kwee IL, and Nakada T (2009) Inhibition of Aquaporin 4 by antiepileptic drugs. Bioorg Med Chem 17: 418-424.","DOI":"10.1016\/j.bmc.2007.12.038"},{"key":"10.1124\/mol.108.053744_bib16","doi-asserted-by":"crossref","unstructured":"Jung JS, Bhat RV, Preston GM, Guggino WB, Baraban JM, and Agre P (1994a) Molecular characterization of an aquaporin cDNA from brain: candidate osmoreceptor and regulator of water balance. Proc Natl Acad Sci U S A 91: 13052-13056.","DOI":"10.1073\/pnas.91.26.13052"},{"key":"10.1124\/mol.108.053744_bib17","doi-asserted-by":"crossref","unstructured":"Jung JS, Preston GM, Smith BL, Guggino WB, and Agre P (1994b) Molecular structure of the water channel through aquaporin CHIP. The hourglass model. J Biol Chem 269: 14648-14654.","DOI":"10.1016\/S0021-9258(17)36674-7"},{"key":"10.1124\/mol.108.053744_bib18","doi-asserted-by":"crossref","unstructured":"Lam TI, Anderson SE, Glaser N, and O\u2019Donnell ME (2005) Bumetanide reduces cerebral edema formation in rats with diabetic ketoacidosis. Diabetes 54: 510-516.","DOI":"10.2337\/diabetes.54.2.510"},{"key":"10.1124\/mol.108.053744_bib19","unstructured":"Ma B, Xiang Y, Mu SM, Li T, Yu HM, and Li XJ (2004) Effects of acetazolamide and anordiol on osmotic water permeability in AQP1-cRNA injected Xenopus oocyte. Acta Pharmacol Sin 25: 90-97."},{"key":"10.1124\/mol.108.053744_bib20","doi-asserted-by":"crossref","unstructured":"Manley GT, Fujimura M, Ma T, Noshita N, Filiz F, Bollen AW, Chan P, and Verkman AS (2000) Aquaporin-4 deletion in mice reduces brain edema after acute water intoxication and ischemic stroke. Nat Med 6: 159-163.","DOI":"10.1038\/72256"},{"key":"10.1124\/mol.108.053744_bib21","doi-asserted-by":"crossref","unstructured":"McClain RM and Dammers KD (1981) Toxicologic evaluation of bumetanide, potent diuretic agent. J Clin Pharmacol 21: 543-554.","DOI":"10.1002\/j.1552-4604.1981.tb05663.x"},{"key":"10.1124\/mol.108.053744_bib22","doi-asserted-by":"crossref","unstructured":"M\u00fcller EM, Hub JS, Grubm\u00fcller H, and de Groot BL (2008) Is TEA an inhibitor for human Aquaporin-1? Pflugers Arch 456: 663-669.","DOI":"10.1007\/s00424-007-0422-0"},{"key":"10.1124\/mol.108.053744_bib23","doi-asserted-by":"crossref","unstructured":"Nico B, Frigeri A, Nicchia GP, Corsi P, Ribatti D, Quondamatteo F, Herken R, Girolamo F, Marzullo A, Svelto M, et al. (2003) Severe alterations of endothelial and glial cells in the blood-brain barrier of dystrophic mdx mice. Glia 42: 235-251.","DOI":"10.1002\/glia.10216"},{"key":"10.1124\/mol.108.053744_bib24","doi-asserted-by":"crossref","unstructured":"Niemietz CM and Tyerman SD (2002) New potent inhibitors of aquaporins: silver and gold compounds inhibit aquaporins of plant and human origin. FEBS letters 531: 443-447.","DOI":"10.1016\/S0014-5793(02)03581-0"},{"key":"10.1124\/mol.108.053744_bib25","doi-asserted-by":"crossref","unstructured":"O\u2019Donnell ME, Tran L, Lam TI, Liu XB, and Anderson SE (2004) Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab 24: 1046-1056.","DOI":"10.1097\/01.WCB.0000130867.32663.90"},{"key":"10.1124\/mol.108.053744_bib26","doi-asserted-by":"crossref","unstructured":"Preston GM, Jung JS, Guggino WB, and Agre P (1993) The mercury-sensitive residue at cysteine 189 in the CHIP28 water channel. J Biol Chem 268: 17-20.","DOI":"10.1016\/S0021-9258(18)54108-9"},{"key":"10.1124\/mol.108.053744_bib27","doi-asserted-by":"crossref","unstructured":"Puwarawuttipanit W, Bragg AD, Frydenlund DS, Mylonakou MN, Nagelhus EA, Peters MF, Kotchabhakdi N, Adams ME, Froehner SC, Haug FM, et al. (2006) Differential effect of alpha-syntrophin knockout on aquaporin-4 and Kir4.1 expression in retinal macroglial cells in mice. Neuroscience 137: 165-175.","DOI":"10.1016\/j.neuroscience.2005.08.051"},{"key":"10.1124\/mol.108.053744_bib28","doi-asserted-by":"crossref","unstructured":"Reizer J, Reizer A, and Saier MH Jr (1993) The MIP family of integral membrane channel proteins: sequence comparisons, evolutionary relationships, reconstructed pathway of evolution, and proposed functional differentiation of the two repeated halves of the proteins. Crit Rev Biochem Mol Biol 28: 235-257.","DOI":"10.3109\/10409239309086796"},{"key":"10.1124\/mol.108.053744_bib29","doi-asserted-by":"crossref","unstructured":"Schlatter E, Greger R, and Weidtke C (1983) Effect of \u201chigh ceiling\u201d diuretics on active salt transport in the cortical thick ascending limb of Henle\u2019s loop of rabbit kidney. Correlation of chemical structure and inhibitory potency. Pflugers Arch 396: 210-217.","DOI":"10.1007\/BF00587857"},{"key":"10.1124\/mol.108.053744_bib30","doi-asserted-by":"crossref","unstructured":"Sui H, Han BG, Lee JK, Walian P, and Jap BK (2001) Structural basis of water-specific transport through the AQP1 water channel. Nature 414: 872-878.","DOI":"10.1038\/414872a"},{"key":"10.1124\/mol.108.053744_bib31","doi-asserted-by":"crossref","unstructured":"Suvitayavat W, Palfrey HC, Haas M, Dunham PB, Kalmar F, and Rao MC (1994) Characterization of the endogenous Na+-K+-2Cl- cotransporter in Xenopus oocytes. Am J Physiol 266: C284-C292.","DOI":"10.1152\/ajpcell.1994.266.1.C284"},{"key":"10.1124\/mol.108.053744_bib32","doi-asserted-by":"crossref","unstructured":"Takeda Y, Koh SD, Sanders KM, and Ward SM (2008) Differential expression of ionic conductances in interstitial cells of Cajal in the murine gastric antrum. J Physiol 586: 859-873.","DOI":"10.1113\/jphysiol.2007.140293"},{"key":"10.1124\/mol.108.053744_bib33","doi-asserted-by":"crossref","unstructured":"T\u00f6rnroth-Horsefield S, Wang Y, Hedfalk K, Johanson U, Karlsson M, Tajkhorshid E, Neutze R, and Kjellbom P (2006) Structural mechanism of plant aquaporin gating. Nature 439: 688-694.","DOI":"10.1038\/nature04316"},{"key":"10.1124\/mol.108.053744_bib34","doi-asserted-by":"crossref","unstructured":"Yang B, Kim JK, and Verkman AS (2006) Comparative efficacy of HgCl2 with candidate aquaporin-1 inhibitors DMSO, gold, TEA+ and acetazolamide. FEBS Lett 580: 6679-6684.","DOI":"10.1016\/j.febslet.2006.11.025"},{"key":"10.1124\/mol.108.053744_bib35","doi-asserted-by":"crossref","unstructured":"Yool AJ, Brokl OH, Pannabecker TL, Dantzler WH, and Stamer WD (2002) Tetraethylammonium block of water flux in Aquaporin-1 channels expressed in kidney thin limbs of Henle\u2019s loop and a kidney-derived cell line. BMC Physiol 2: 4.","DOI":"10.1186\/1472-6793-2-4"},{"key":"10.1124\/mol.108.053744_bib36","doi-asserted-by":"crossref","unstructured":"Yool AJ (2007a) Aquaporins: multiple roles in the central nervous system. Neuroscientist 13: 470-485.","DOI":"10.1177\/1073858407303081"},{"key":"10.1124\/mol.108.053744_bib37","doi-asserted-by":"crossref","unstructured":"Yool AJ (2007b) Functional domains of aquaporin-1: keys to physiology, and targets for drug discovery. Curr Pharm Des 13: 3212-3221.","DOI":"10.2174\/138161207782341349"},{"key":"10.1124\/mol.108.053744_bib38","doi-asserted-by":"crossref","unstructured":"Yu J, Yool AJ, Schulten K, and Tajkhorshid E (2006) Mechanism of gating and ion conductivity of a possible tetrameric pore in aquaporin-1. Structure 14: 1411-1423.","DOI":"10.1016\/j.str.2006.07.006"},{"key":"10.1124\/mol.108.053744_bib39","doi-asserted-by":"crossref","unstructured":"Zelenina M, Zelenin S, Bondar AA, Brismar H, and Aperia A (2002) Water permeability of aquaporin-4 is decreased by protein kinase C and dopamine. Am J Physiol Renal Physiol 283: F309-F318.","DOI":"10.1152\/ajprenal.00260.2001"}],"container-title":["Molecular Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0026895X24019758?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0026895X24019758?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/syndication.highwire.org\/content\/doi\/10.1124\/mol.108.053744","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,2,19]],"date-time":"2025-02-19T09:36:28Z","timestamp":1739957788000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0026895X24019758"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2009,7]]},"references-count":39,"journal-issue":{"issue":"1","published-print":{"date-parts":[[2009,7]]}},"alternative-id":["S0026895X24019758"],"URL":"https:\/\/doi.org\/10.1124\/mol.108.053744","relation":{},"ISSN":["0026-895X"],"issn-type":[{"value":"0026-895X","type":"print"}],"subject":[],"published":{"date-parts":[[2009,7]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Inhibition of Aquaporin-1 and Aquaporin-4 Water Permeability by a Derivative of the Loop Diuretic Bumetanide Acting at an Internal Pore-Occluding Binding Site","name":"articletitle","label":"Article Title"},{"value":"Molecular Pharmacology","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1124\/mol.108.053744","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2009 The American Society for Pharmacology and Experimental Therapeutics","name":"copyright","label":"Copyright"}]}}