Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using 11C‐MDG
Sodium‐dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 1...
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| Veröffentlicht in: | Pharmacology research & perspectives 2016-08, Vol.4 (4), p.e00244-n/a |
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| creator | Mitsuoka, Keisuke Hayashizaki, Yuka Murakami, Yoshihiro Takasu, Toshiyuki Yokono, Masanori Umeda, Nobuhiro Takakura, Shoji Noda, Akihiro Miyoshi, Sosuke |
| description | Sodium‐dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C‐methyl‐d‐glucoside (11C‐MDG), an SGLT‐specific radio‐labeled substrate. PET imaging with 11C‐MDG in vehicle‐treated rats demonstrated that intravenously injected 11C‐MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLTs. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of 11C‐MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of 11C‐MDG. This method of visualizing the mode of action of an SGLT2 inhibitor in vivo has demonstrated the drug's mechanism in reducing renal glucose reabsorption in kidney in living animals. |
| doi_str_mv | 10.1002/prp2.244 |
| format | Article |
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The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C‐methyl‐d‐glucoside (11C‐MDG), an SGLT‐specific radio‐labeled substrate. PET imaging with 11C‐MDG in vehicle‐treated rats demonstrated that intravenously injected 11C‐MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLTs. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of 11C‐MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of 11C‐MDG. 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The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C‐methyl‐d‐glucoside (11C‐MDG), an SGLT‐specific radio‐labeled substrate. PET imaging with 11C‐MDG in vehicle‐treated rats demonstrated that intravenously injected 11C‐MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLTs. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of 11C‐MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of 11C‐MDG. This method of visualizing the mode of action of an SGLT2 inhibitor in vivo has demonstrated the drug's mechanism in reducing renal glucose reabsorption in kidney in living animals.</description><subject>Ipragliflozin and visualization</subject><subject>MDG</subject><subject>Original</subject><subject>PET</subject><subject>SGLT2</subject><issn>2052-1707</issn><issn>2052-1707</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>24P</sourceid><recordid>eNpVUctOwzAQtBCIVqUSn5AjlxSv4zjtBQmVtiAVUUE5W47rpK6cOORRVE58At_Il-DQqoI97K40o9nHIHQJeAAYk-uiLMiAUHqCugSHxIcIR6d_-g7qV9UGYwxAMQTkHHXIEIDhUdRF2bTJZa1tLoynM5HqPPVs4hVrUWZCWmNTLR0kfjkt8jKbL4mn87WOdW1LTxelSI1OjP3QubfVwltMlkeppmozwPj78-vxbnaBzhJhKtU_1B56nU6W43t__jR7GN_O_Q0hjPqKMKUYxGFAGQEZCkioCiVN4kgBZgGOY6ZIFCp3HmWBoNLFilIsV4lkIxH00M1et2jiTK2kyutSGF6Ubq9yx63Q_D-S6zVP7ZaHhBJgIydwdRAo7VujqppnupLKGJEr21Qchsw9MGIsclR_T33XRu2OMwDz1h3eusOdO3zxvCCuBj8LDoSD</recordid><startdate>201608</startdate><enddate>201608</enddate><creator>Mitsuoka, Keisuke</creator><creator>Hayashizaki, Yuka</creator><creator>Murakami, Yoshihiro</creator><creator>Takasu, Toshiyuki</creator><creator>Yokono, Masanori</creator><creator>Umeda, Nobuhiro</creator><creator>Takakura, Shoji</creator><creator>Noda, Akihiro</creator><creator>Miyoshi, Sosuke</creator><general>John Wiley and Sons Inc</general><scope>24P</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>201608</creationdate><title>Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using 11C‐MDG</title><author>Mitsuoka, Keisuke ; Hayashizaki, Yuka ; Murakami, Yoshihiro ; Takasu, Toshiyuki ; Yokono, Masanori ; Umeda, Nobuhiro ; Takakura, Shoji ; Noda, Akihiro ; Miyoshi, Sosuke</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j2264-e26ee61b534621c5a1f4e5c4fb7e10630bb6e275e170463a4ccccd440cdfc69a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Ipragliflozin and visualization</topic><topic>MDG</topic><topic>Original</topic><topic>PET</topic><topic>SGLT2</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mitsuoka, Keisuke</creatorcontrib><creatorcontrib>Hayashizaki, Yuka</creatorcontrib><creatorcontrib>Murakami, Yoshihiro</creatorcontrib><creatorcontrib>Takasu, Toshiyuki</creatorcontrib><creatorcontrib>Yokono, Masanori</creatorcontrib><creatorcontrib>Umeda, Nobuhiro</creatorcontrib><creatorcontrib>Takakura, Shoji</creatorcontrib><creatorcontrib>Noda, Akihiro</creatorcontrib><creatorcontrib>Miyoshi, Sosuke</creatorcontrib><collection>Wiley Online Library Open Access</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Pharmacology research & perspectives</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mitsuoka, Keisuke</au><au>Hayashizaki, Yuka</au><au>Murakami, Yoshihiro</au><au>Takasu, Toshiyuki</au><au>Yokono, Masanori</au><au>Umeda, Nobuhiro</au><au>Takakura, Shoji</au><au>Noda, Akihiro</au><au>Miyoshi, Sosuke</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using 11C‐MDG</atitle><jtitle>Pharmacology research & perspectives</jtitle><date>2016-08</date><risdate>2016</risdate><volume>4</volume><issue>4</issue><spage>e00244</spage><epage>n/a</epage><pages>e00244-n/a</pages><issn>2052-1707</issn><eissn>2052-1707</eissn><abstract>Sodium‐dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C‐methyl‐d‐glucoside (11C‐MDG), an SGLT‐specific radio‐labeled substrate. PET imaging with 11C‐MDG in vehicle‐treated rats demonstrated that intravenously injected 11C‐MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLTs. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of 11C‐MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of 11C‐MDG. This method of visualizing the mode of action of an SGLT2 inhibitor in vivo has demonstrated the drug's mechanism in reducing renal glucose reabsorption in kidney in living animals.</abstract><cop>Hoboken</cop><pub>John Wiley and Sons Inc</pub><pmid>28116097</pmid><doi>10.1002/prp2.244</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| source | Wiley Online Library Open Access; DOAJ Directory of Open Access Journals; Wiley Online Library Journals Frontfile Complete; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central |
| subjects | Ipragliflozin and visualization MDG Original PET SGLT2 |
| title | Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using 11C‐MDG |
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