Characterization of endothelin receptors in streptozotocin-induced diabetic rat vas deferens
As there is increasing evidence that diabetes induces changes in the plasma levels of endothelins (ETs) and in the properties of ET receptors in peripheral tissues, and as there are reports indicating the presence of significant amounts of ET receptors in mammalian vasa deferentia, we studied possib...
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Veröffentlicht in: | Biochemical pharmacology 1996-11, Vol.52 (10), p.1593-1598 |
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description | As there is increasing evidence that diabetes induces changes in the plasma levels of endothelins (ETs) and in the properties of ET receptors in peripheral tissues, and as there are reports indicating the presence of significant amounts of ET receptors in mammalian vasa deferentia, we studied possible alterations in ET receptor characteristics in the vasa deferentia of the following groups of rats: 8 weeks diabetic (D
8), 8 weeks age-matched control (C
8), 16 weeks diabetic (D
16), 16 weeks diabetic-insulin-treated (started 8 weeks after the onset of diabetes) (DI
16), and 16 weeks age-matched control (C
16). Diabetes was induced by the i.v. injection of 65 mg/kg streptozotocin (STZ). Diabetic rats had hyperglycemia, hypoinsulinemia, glucosuria, polydipsia, and polyuria and had smaller vasa deferentia than control and diabetic-insulin-treated animals. Receptor binding experiments with [
125I]ET-1 demonstrated that the densities of ET receptors in vasa deferentia from D
8, C
8, D
16, DI
16, and C
16 animals were 377 ± 11, 255 ± 24, 315 ± 18, 210 ± 12, and 214 ± 7 fmol/mg of protein, respectively. [
125I]ET-1 binding to the ET receptors was inhibited by ET-1 (non-selective), BQ 610 (ET
A selective), ET-3 (ET
C selective), and IRL 1620 (ET
B selective) with the following rank order of
K
i
values: ET-1 < BQ 610 < ET-3 ⪡ IRL 1620. The pharmacological profile of the ET receptors was similar in all groups and was consistent with the predominance of the ET
A receptor subtype in the rat vasa deferentia. Our data indicate that experimental diabetes up-regulates the density of ET receptors in the rat vasa deferentia and that the receptor up-regulation is reversed by insulin treatment. |
doi_str_mv | 10.1016/S0006-2952(96)00565-5 |
format | Article |
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8), 8 weeks age-matched control (C
8), 16 weeks diabetic (D
16), 16 weeks diabetic-insulin-treated (started 8 weeks after the onset of diabetes) (DI
16), and 16 weeks age-matched control (C
16). Diabetes was induced by the i.v. injection of 65 mg/kg streptozotocin (STZ). Diabetic rats had hyperglycemia, hypoinsulinemia, glucosuria, polydipsia, and polyuria and had smaller vasa deferentia than control and diabetic-insulin-treated animals. Receptor binding experiments with [
125I]ET-1 demonstrated that the densities of ET receptors in vasa deferentia from D
8, C
8, D
16, DI
16, and C
16 animals were 377 ± 11, 255 ± 24, 315 ± 18, 210 ± 12, and 214 ± 7 fmol/mg of protein, respectively. [
125I]ET-1 binding to the ET receptors was inhibited by ET-1 (non-selective), BQ 610 (ET
A selective), ET-3 (ET
C selective), and IRL 1620 (ET
B selective) with the following rank order of
K
i
values: ET-1 < BQ 610 < ET-3 ⪡ IRL 1620. The pharmacological profile of the ET receptors was similar in all groups and was consistent with the predominance of the ET
A receptor subtype in the rat vasa deferentia. Our data indicate that experimental diabetes up-regulates the density of ET receptors in the rat vasa deferentia and that the receptor up-regulation is reversed by insulin treatment.</description><identifier>ISSN: 0006-2952</identifier><identifier>EISSN: 1873-2968</identifier><identifier>DOI: 10.1016/S0006-2952(96)00565-5</identifier><identifier>PMID: 8937475</identifier><identifier>CODEN: BCPCA6</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Animals ; Biological and medical sciences ; diabetes ; Diabetes Mellitus, Experimental - drug therapy ; Diabetes Mellitus, Experimental - metabolism ; Diabetes. Impaired glucose tolerance ; Endocrine pancreas. Apud cells (diseases) ; Endocrinopathies ; endothelin receptors ; Endothelin-1 - antagonists & inhibitors ; Endothelin-1 - metabolism ; Endothelin-1 - pharmacology ; Endothelins - pharmacology ; Etiopathogenesis. Screening. Investigations. Target tissue resistance ; Insulin - therapeutic use ; Kinetics ; Male ; Medical sciences ; Oligopeptides - pharmacology ; Peptide Fragments - pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Endothelin A ; Receptor, Endothelin B ; Receptors, Endothelin - drug effects ; Receptors, Endothelin - metabolism ; Time Factors ; Up-Regulation ; vas deferens ; Vas Deferens - drug effects ; Vas Deferens - metabolism</subject><ispartof>Biochemical pharmacology, 1996-11, Vol.52 (10), p.1593-1598</ispartof><rights>1996</rights><rights>1997 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c436t-b3e3b91e7cd1f3dcd84e5c8dddf6728f7cf22437e56cdb72b05f1443df51ff2c3</citedby><cites>FETCH-LOGICAL-c436t-b3e3b91e7cd1f3dcd84e5c8dddf6728f7cf22437e56cdb72b05f1443df51ff2c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0006-2952(96)00565-5$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2494432$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8937475$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Saito, Motoaki</creatorcontrib><creatorcontrib>Nishi, Kazuhiko</creatorcontrib><creatorcontrib>Fukumoto, Yuji</creatorcontrib><creatorcontrib>Weiss, Robert M.</creatorcontrib><creatorcontrib>Latifpour, Jamshid</creatorcontrib><title>Characterization of endothelin receptors in streptozotocin-induced diabetic rat vas deferens</title><title>Biochemical pharmacology</title><addtitle>Biochem Pharmacol</addtitle><description>As there is increasing evidence that diabetes induces changes in the plasma levels of endothelins (ETs) and in the properties of ET receptors in peripheral tissues, and as there are reports indicating the presence of significant amounts of ET receptors in mammalian vasa deferentia, we studied possible alterations in ET receptor characteristics in the vasa deferentia of the following groups of rats: 8 weeks diabetic (D
8), 8 weeks age-matched control (C
8), 16 weeks diabetic (D
16), 16 weeks diabetic-insulin-treated (started 8 weeks after the onset of diabetes) (DI
16), and 16 weeks age-matched control (C
16). Diabetes was induced by the i.v. injection of 65 mg/kg streptozotocin (STZ). Diabetic rats had hyperglycemia, hypoinsulinemia, glucosuria, polydipsia, and polyuria and had smaller vasa deferentia than control and diabetic-insulin-treated animals. Receptor binding experiments with [
125I]ET-1 demonstrated that the densities of ET receptors in vasa deferentia from D
8, C
8, D
16, DI
16, and C
16 animals were 377 ± 11, 255 ± 24, 315 ± 18, 210 ± 12, and 214 ± 7 fmol/mg of protein, respectively. [
125I]ET-1 binding to the ET receptors was inhibited by ET-1 (non-selective), BQ 610 (ET
A selective), ET-3 (ET
C selective), and IRL 1620 (ET
B selective) with the following rank order of
K
i
values: ET-1 < BQ 610 < ET-3 ⪡ IRL 1620. The pharmacological profile of the ET receptors was similar in all groups and was consistent with the predominance of the ET
A receptor subtype in the rat vasa deferentia. Our data indicate that experimental diabetes up-regulates the density of ET receptors in the rat vasa deferentia and that the receptor up-regulation is reversed by insulin treatment.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>diabetes</subject><subject>Diabetes Mellitus, Experimental - drug therapy</subject><subject>Diabetes Mellitus, Experimental - metabolism</subject><subject>Diabetes. Impaired glucose tolerance</subject><subject>Endocrine pancreas. Apud cells (diseases)</subject><subject>Endocrinopathies</subject><subject>endothelin receptors</subject><subject>Endothelin-1 - antagonists & inhibitors</subject><subject>Endothelin-1 - metabolism</subject><subject>Endothelin-1 - pharmacology</subject><subject>Endothelins - pharmacology</subject><subject>Etiopathogenesis. Screening. Investigations. Target tissue resistance</subject><subject>Insulin - therapeutic use</subject><subject>Kinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Oligopeptides - pharmacology</subject><subject>Peptide Fragments - pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptor, Endothelin A</subject><subject>Receptor, Endothelin B</subject><subject>Receptors, Endothelin - drug effects</subject><subject>Receptors, Endothelin - metabolism</subject><subject>Time Factors</subject><subject>Up-Regulation</subject><subject>vas deferens</subject><subject>Vas Deferens - drug effects</subject><subject>Vas Deferens - metabolism</subject><issn>0006-2952</issn><issn>1873-2968</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1rGzEQhkVpSZy0PyGwh1CSw7b6WH3sKRSTj0Kgh7S3gtBKI6KylhxJDjS_PnJsfM1peGeekYYHoTOCvxFMxPcHjLHo6cjpxSguMeaC9_wDWhAlWWsL9REtDsgxOinl3zYqQY7QkRqZHCRfoL_LR5ONrZDDi6khxS75DqJL9RHmELsMFtY15dK1UGrehpdUkw2xD9FtLLjOBTNBDbbLpnbPpnQOPGSI5TP65M1c4Mu-nqI_N9e_l3f9_a_bn8sf970dmKj9xIBNIwFpHfHMWacG4FY557yQVHlpPaUDk8CFdZOkE-aeDANznhPvqWWn6Ovu3XVOTxsoVa9CsTDPJkLaFC0VF1jxoYF8B9qcSsng9TqHlcn_NcF6a1W_WdVbZXoU-s2q5m3vbP_BZlqBO2ztNbb5-X5uijWzzybaUA4YHcZ2Lm3Y1Q6DJuM5QNbFBojNYWieq3YpvHPIKxzslm4</recordid><startdate>19961122</startdate><enddate>19961122</enddate><creator>Saito, Motoaki</creator><creator>Nishi, Kazuhiko</creator><creator>Fukumoto, Yuji</creator><creator>Weiss, Robert M.</creator><creator>Latifpour, Jamshid</creator><general>Elsevier Inc</general><general>Elsevier Science</general><scope>IQODW</scope><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>7X8</scope></search><sort><creationdate>19961122</creationdate><title>Characterization of endothelin receptors in streptozotocin-induced diabetic rat vas deferens</title><author>Saito, Motoaki ; Nishi, Kazuhiko ; Fukumoto, Yuji ; Weiss, Robert M. ; Latifpour, Jamshid</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c436t-b3e3b91e7cd1f3dcd84e5c8dddf6728f7cf22437e56cdb72b05f1443df51ff2c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>diabetes</topic><topic>Diabetes Mellitus, Experimental - drug therapy</topic><topic>Diabetes Mellitus, Experimental - metabolism</topic><topic>Diabetes. Impaired glucose tolerance</topic><topic>Endocrine pancreas. Apud cells (diseases)</topic><topic>Endocrinopathies</topic><topic>endothelin receptors</topic><topic>Endothelin-1 - antagonists & inhibitors</topic><topic>Endothelin-1 - metabolism</topic><topic>Endothelin-1 - pharmacology</topic><topic>Endothelins - pharmacology</topic><topic>Etiopathogenesis. Screening. Investigations. Target tissue resistance</topic><topic>Insulin - therapeutic use</topic><topic>Kinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Oligopeptides - pharmacology</topic><topic>Peptide Fragments - pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptor, Endothelin A</topic><topic>Receptor, Endothelin B</topic><topic>Receptors, Endothelin - drug effects</topic><topic>Receptors, Endothelin - metabolism</topic><topic>Time Factors</topic><topic>Up-Regulation</topic><topic>vas deferens</topic><topic>Vas Deferens - drug effects</topic><topic>Vas Deferens - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Saito, Motoaki</creatorcontrib><creatorcontrib>Nishi, Kazuhiko</creatorcontrib><creatorcontrib>Fukumoto, Yuji</creatorcontrib><creatorcontrib>Weiss, Robert M.</creatorcontrib><creatorcontrib>Latifpour, Jamshid</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Biochemical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Saito, Motoaki</au><au>Nishi, Kazuhiko</au><au>Fukumoto, Yuji</au><au>Weiss, Robert M.</au><au>Latifpour, Jamshid</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characterization of endothelin receptors in streptozotocin-induced diabetic rat vas deferens</atitle><jtitle>Biochemical pharmacology</jtitle><addtitle>Biochem Pharmacol</addtitle><date>1996-11-22</date><risdate>1996</risdate><volume>52</volume><issue>10</issue><spage>1593</spage><epage>1598</epage><pages>1593-1598</pages><issn>0006-2952</issn><eissn>1873-2968</eissn><coden>BCPCA6</coden><abstract>As there is increasing evidence that diabetes induces changes in the plasma levels of endothelins (ETs) and in the properties of ET receptors in peripheral tissues, and as there are reports indicating the presence of significant amounts of ET receptors in mammalian vasa deferentia, we studied possible alterations in ET receptor characteristics in the vasa deferentia of the following groups of rats: 8 weeks diabetic (D
8), 8 weeks age-matched control (C
8), 16 weeks diabetic (D
16), 16 weeks diabetic-insulin-treated (started 8 weeks after the onset of diabetes) (DI
16), and 16 weeks age-matched control (C
16). Diabetes was induced by the i.v. injection of 65 mg/kg streptozotocin (STZ). Diabetic rats had hyperglycemia, hypoinsulinemia, glucosuria, polydipsia, and polyuria and had smaller vasa deferentia than control and diabetic-insulin-treated animals. Receptor binding experiments with [
125I]ET-1 demonstrated that the densities of ET receptors in vasa deferentia from D
8, C
8, D
16, DI
16, and C
16 animals were 377 ± 11, 255 ± 24, 315 ± 18, 210 ± 12, and 214 ± 7 fmol/mg of protein, respectively. [
125I]ET-1 binding to the ET receptors was inhibited by ET-1 (non-selective), BQ 610 (ET
A selective), ET-3 (ET
C selective), and IRL 1620 (ET
B selective) with the following rank order of
K
i
values: ET-1 < BQ 610 < ET-3 ⪡ IRL 1620. The pharmacological profile of the ET receptors was similar in all groups and was consistent with the predominance of the ET
A receptor subtype in the rat vasa deferentia. Our data indicate that experimental diabetes up-regulates the density of ET receptors in the rat vasa deferentia and that the receptor up-regulation is reversed by insulin treatment.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>8937475</pmid><doi>10.1016/S0006-2952(96)00565-5</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Animals Biological and medical sciences diabetes Diabetes Mellitus, Experimental - drug therapy Diabetes Mellitus, Experimental - metabolism Diabetes. Impaired glucose tolerance Endocrine pancreas. Apud cells (diseases) Endocrinopathies endothelin receptors Endothelin-1 - antagonists & inhibitors Endothelin-1 - metabolism Endothelin-1 - pharmacology Endothelins - pharmacology Etiopathogenesis. Screening. Investigations. Target tissue resistance Insulin - therapeutic use Kinetics Male Medical sciences Oligopeptides - pharmacology Peptide Fragments - pharmacology Rats Rats, Sprague-Dawley Receptor, Endothelin A Receptor, Endothelin B Receptors, Endothelin - drug effects Receptors, Endothelin - metabolism Time Factors Up-Regulation vas deferens Vas Deferens - drug effects Vas Deferens - metabolism |
title | Characterization of endothelin receptors in streptozotocin-induced diabetic rat vas deferens |
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