S3226, a novel inhibitor of Na+/H+ exchanger subtype 3 in various cell types
Inhibition of Na+/H+ exchange (NHE) subtypes has been investigated in a study of the mouse fibroblast L cell line (LAP1) transfected with human (h) NHE1, rabbit (rb) NHE2, rat (rt) or human (h) NHE3 as well as an opossum kidney cell line (OK) and porcine renal brush-border membrane vesicles (BBMV)....
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| Veröffentlicht in: | Pflügers Archiv 1998-10, Vol.436 (5), p.797-800 |
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| creator | Schwark, J R Jansen, H W Lang, H J Krick, W Burckhardt, G Hropot, M |
| description | Inhibition of Na+/H+ exchange (NHE) subtypes has been investigated in a study of the mouse fibroblast L cell line (LAP1) transfected with human (h) NHE1, rabbit (rb) NHE2, rat (rt) or human (h) NHE3 as well as an opossum kidney cell line (OK) and porcine renal brush-border membrane vesicles (BBMV). S3226 ¿3-[2-(3-guanidino-2-methyl-3-oxo-propenyl)-5-methyl-phenyl]-N-isopro pylidene-2-methyl-acrylamide dihydro-chloride¿ was the most potent and specific NHE3 inhibitor with an IC50 value of 0.02 micromol/l for the human isoform, whereas its IC50 value for hNHE1 and rbNHE2 was 3.6 and approximately = 80 micromol/l, respectively. In contrast, amiloride is a weak NHE3 inhibitor (IC50>100 micromol/l) with a higher affinity to hNHE1 and rbNHE2. Cariporide (4-isopropyl-3-methylsulphonyl-benzoyl-guanidine methane-sulphonate), which has an IC50 for NHE3 of approximately 1 mmol/l, is a highly selective NHE1 inhibitor (0.08 micromol/l). Therefore, S3226 is a novel tool with which to investigate the physiological and pathophysiological roles of NHE3 in animal models. |
| doi_str_mv | 10.1007/s004240050704 |
| format | Article |
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S3226 ¿3-[2-(3-guanidino-2-methyl-3-oxo-propenyl)-5-methyl-phenyl]-N-isopro pylidene-2-methyl-acrylamide dihydro-chloride¿ was the most potent and specific NHE3 inhibitor with an IC50 value of 0.02 micromol/l for the human isoform, whereas its IC50 value for hNHE1 and rbNHE2 was 3.6 and approximately = 80 micromol/l, respectively. In contrast, amiloride is a weak NHE3 inhibitor (IC50>100 micromol/l) with a higher affinity to hNHE1 and rbNHE2. Cariporide (4-isopropyl-3-methylsulphonyl-benzoyl-guanidine methane-sulphonate), which has an IC50 for NHE3 of approximately 1 mmol/l, is a highly selective NHE1 inhibitor (0.08 micromol/l). Therefore, S3226 is a novel tool with which to investigate the physiological and pathophysiological roles of NHE3 in animal models.</description><identifier>ISSN: 0031-6768</identifier><identifier>EISSN: 1432-2013</identifier><identifier>DOI: 10.1007/s004240050704</identifier><identifier>PMID: 9716715</identifier><language>eng</language><publisher>Germany: Springer Nature B.V</publisher><subject>Amiloride - pharmacology ; Animals ; Cell Line ; Dose-Response Relationship, Drug ; Guanidines - metabolism ; Guanidines - pharmacology ; Humans ; Ion Channels - antagonists & inhibitors ; Methacrylates - metabolism ; Methacrylates - pharmacology ; Mice ; Microvilli - drug effects ; Opossums ; Proteins ; Rabbits ; Rats ; Rodents ; Small intestine ; Sodium-Hydrogen Exchanger 3 ; Sodium-Hydrogen Exchangers - antagonists & inhibitors ; Stereoisomerism ; Studies ; Sulfones - pharmacology ; Swine</subject><ispartof>Pflügers Archiv, 1998-10, Vol.436 (5), p.797-800</ispartof><rights>Springer-Verlag Berlin Heidelberg 1998</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c381t-affd1c5e7cf13f4a0a1aad9d03da165036573b503a3f911f184a499b5368ced33</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9716715$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Schwark, J R</creatorcontrib><creatorcontrib>Jansen, H W</creatorcontrib><creatorcontrib>Lang, H J</creatorcontrib><creatorcontrib>Krick, W</creatorcontrib><creatorcontrib>Burckhardt, G</creatorcontrib><creatorcontrib>Hropot, M</creatorcontrib><title>S3226, a novel inhibitor of Na+/H+ exchanger subtype 3 in various cell types</title><title>Pflügers Archiv</title><addtitle>Pflugers Arch</addtitle><description>Inhibition of Na+/H+ exchange (NHE) subtypes has been investigated in a study of the mouse fibroblast L cell line (LAP1) transfected with human (h) NHE1, rabbit (rb) NHE2, rat (rt) or human (h) NHE3 as well as an opossum kidney cell line (OK) and porcine renal brush-border membrane vesicles (BBMV). S3226 ¿3-[2-(3-guanidino-2-methyl-3-oxo-propenyl)-5-methyl-phenyl]-N-isopro pylidene-2-methyl-acrylamide dihydro-chloride¿ was the most potent and specific NHE3 inhibitor with an IC50 value of 0.02 micromol/l for the human isoform, whereas its IC50 value for hNHE1 and rbNHE2 was 3.6 and approximately = 80 micromol/l, respectively. In contrast, amiloride is a weak NHE3 inhibitor (IC50>100 micromol/l) with a higher affinity to hNHE1 and rbNHE2. Cariporide (4-isopropyl-3-methylsulphonyl-benzoyl-guanidine methane-sulphonate), which has an IC50 for NHE3 of approximately 1 mmol/l, is a highly selective NHE1 inhibitor (0.08 micromol/l). Therefore, S3226 is a novel tool with which to investigate the physiological and pathophysiological roles of NHE3 in animal models.</description><subject>Amiloride - pharmacology</subject><subject>Animals</subject><subject>Cell Line</subject><subject>Dose-Response Relationship, Drug</subject><subject>Guanidines - metabolism</subject><subject>Guanidines - pharmacology</subject><subject>Humans</subject><subject>Ion Channels - antagonists & inhibitors</subject><subject>Methacrylates - metabolism</subject><subject>Methacrylates - pharmacology</subject><subject>Mice</subject><subject>Microvilli - drug effects</subject><subject>Opossums</subject><subject>Proteins</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Rodents</subject><subject>Small intestine</subject><subject>Sodium-Hydrogen Exchanger 3</subject><subject>Sodium-Hydrogen Exchangers - antagonists & inhibitors</subject><subject>Stereoisomerism</subject><subject>Studies</subject><subject>Sulfones - pharmacology</subject><subject>Swine</subject><issn>0031-6768</issn><issn>1432-2013</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNpdkEFLw0AQhRdRaq0ePQqLBy81dmZnk02OUtQKRQ_qOWySXZuSJnU3Kfbfm9IiKHN4MHw8Ph5jlwh3CKAmHkAKCRCCAnnEhihJBAKQjtkQgDCIVBSfsjPvlwAgZCwGbJAojBSGQzZ_IyGiW6553WxMxct6UWZl2zjeWP6ix5PZmJvvfKHrT-O477J2uzaceo5vtCubzvPcVBXfvf05O7G68ubikCP28fjwPp0F89en5-n9PMgpxjbQ1haYh0blFslKDRq1LpICqNAYhUBRqCjrU5NNEC3GUsskyUKK4twURCN2s-9du-arM75NV6Xfaeja9EapolgqIZIevP4HLpvO1b1bGisJgqL-RizYQ7lrvHfGpmtXrrTbpgjpbuL0z8Q9f3Uo7bKVKX7pw6b0A00rcws</recordid><startdate>19981001</startdate><enddate>19981001</enddate><creator>Schwark, J R</creator><creator>Jansen, H W</creator><creator>Lang, H J</creator><creator>Krick, W</creator><creator>Burckhardt, G</creator><creator>Hropot, M</creator><general>Springer Nature B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7QP</scope><scope>7TK</scope><scope>7TS</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88E</scope><scope>8AO</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>7X8</scope></search><sort><creationdate>19981001</creationdate><title>S3226, a novel inhibitor of Na+/H+ exchanger subtype 3 in various cell types</title><author>Schwark, J R ; Jansen, H W ; Lang, H J ; Krick, W ; Burckhardt, G ; Hropot, M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c381t-affd1c5e7cf13f4a0a1aad9d03da165036573b503a3f911f184a499b5368ced33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Amiloride - pharmacology</topic><topic>Animals</topic><topic>Cell Line</topic><topic>Dose-Response Relationship, Drug</topic><topic>Guanidines - metabolism</topic><topic>Guanidines - pharmacology</topic><topic>Humans</topic><topic>Ion Channels - antagonists & inhibitors</topic><topic>Methacrylates - metabolism</topic><topic>Methacrylates - pharmacology</topic><topic>Mice</topic><topic>Microvilli - drug effects</topic><topic>Opossums</topic><topic>Proteins</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Rodents</topic><topic>Small intestine</topic><topic>Sodium-Hydrogen Exchanger 3</topic><topic>Sodium-Hydrogen Exchangers - antagonists & inhibitors</topic><topic>Stereoisomerism</topic><topic>Studies</topic><topic>Sulfones - pharmacology</topic><topic>Swine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Schwark, J R</creatorcontrib><creatorcontrib>Jansen, H W</creatorcontrib><creatorcontrib>Lang, H J</creatorcontrib><creatorcontrib>Krick, W</creatorcontrib><creatorcontrib>Burckhardt, G</creatorcontrib><creatorcontrib>Hropot, M</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Physical Education Index</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Biology Database (Alumni Edition)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Biological Science Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>MEDLINE - Academic</collection><jtitle>Pflügers Archiv</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Schwark, J R</au><au>Jansen, H W</au><au>Lang, H J</au><au>Krick, W</au><au>Burckhardt, G</au><au>Hropot, M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>S3226, a novel inhibitor of Na+/H+ exchanger subtype 3 in various cell types</atitle><jtitle>Pflügers Archiv</jtitle><addtitle>Pflugers Arch</addtitle><date>1998-10-01</date><risdate>1998</risdate><volume>436</volume><issue>5</issue><spage>797</spage><epage>800</epage><pages>797-800</pages><issn>0031-6768</issn><eissn>1432-2013</eissn><abstract>Inhibition of Na+/H+ exchange (NHE) subtypes has been investigated in a study of the mouse fibroblast L cell line (LAP1) transfected with human (h) NHE1, rabbit (rb) NHE2, rat (rt) or human (h) NHE3 as well as an opossum kidney cell line (OK) and porcine renal brush-border membrane vesicles (BBMV). S3226 ¿3-[2-(3-guanidino-2-methyl-3-oxo-propenyl)-5-methyl-phenyl]-N-isopro pylidene-2-methyl-acrylamide dihydro-chloride¿ was the most potent and specific NHE3 inhibitor with an IC50 value of 0.02 micromol/l for the human isoform, whereas its IC50 value for hNHE1 and rbNHE2 was 3.6 and approximately = 80 micromol/l, respectively. In contrast, amiloride is a weak NHE3 inhibitor (IC50>100 micromol/l) with a higher affinity to hNHE1 and rbNHE2. Cariporide (4-isopropyl-3-methylsulphonyl-benzoyl-guanidine methane-sulphonate), which has an IC50 for NHE3 of approximately 1 mmol/l, is a highly selective NHE1 inhibitor (0.08 micromol/l). Therefore, S3226 is a novel tool with which to investigate the physiological and pathophysiological roles of NHE3 in animal models.</abstract><cop>Germany</cop><pub>Springer Nature B.V</pub><pmid>9716715</pmid><doi>10.1007/s004240050704</doi><tpages>4</tpages></addata></record> |
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| subjects | Amiloride - pharmacology Animals Cell Line Dose-Response Relationship, Drug Guanidines - metabolism Guanidines - pharmacology Humans Ion Channels - antagonists & inhibitors Methacrylates - metabolism Methacrylates - pharmacology Mice Microvilli - drug effects Opossums Proteins Rabbits Rats Rodents Small intestine Sodium-Hydrogen Exchanger 3 Sodium-Hydrogen Exchangers - antagonists & inhibitors Stereoisomerism Studies Sulfones - pharmacology Swine |
| title | S3226, a novel inhibitor of Na+/H+ exchanger subtype 3 in various cell types |
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