In vitro effects of strontium ranelate on the extracellular calcium-sensing receptor
The extracellular calcium-sensing receptor (CaSR) is activated by divalent cations and might mediate some of the effects of strontium ranelate, a new drug for the prevention and treatment of post-menopausal osteoporosis. Here, we showed that the maximal effect of Sr 2+ was comparable to that observe...
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| Veröffentlicht in: | Biochemical and biophysical research communications 2004-10, Vol.323 (4), p.1184-1190 |
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| creator | Coulombe, Josée Faure, Hélène Robin, Bruno Ruat, Martial |
| description | The extracellular calcium-sensing receptor (CaSR) is activated by divalent cations and might mediate some of the effects of strontium ranelate, a new drug for the prevention and treatment of post-menopausal osteoporosis. Here, we showed that the maximal effect of Sr
2+ was comparable to that observed for Ca
2+ for both the cloned rat CaSR expressed in Chinese hamster ovary [CHO(CaSR)] cells and the mouse CaSR constitutively expressed in AtT-20 cells as measured by the accumulation of [
3H]inositol phosphates (IP) resulting from CaSR activation. Strontium ranelate also displayed comparable agonist activity for the CaSR in both cell lines. Sodium ranelate did not stimulate the IP response in CHO(CaSR) cells. The IP response resulting from activation of other G-protein-coupled receptors was potentiated by Sr
2+, suggesting that entry of Sr
2+ into the cells might influence phospholipase C activity. Modulation of the CaSR activity in bone cells by strontium ranelate may contribute to its reported antiosteoporotic effects. |
| doi_str_mv | 10.1016/j.bbrc.2004.08.209 |
| format | Article |
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2+ for both the cloned rat CaSR expressed in Chinese hamster ovary [CHO(CaSR)] cells and the mouse CaSR constitutively expressed in AtT-20 cells as measured by the accumulation of [
3H]inositol phosphates (IP) resulting from CaSR activation. Strontium ranelate also displayed comparable agonist activity for the CaSR in both cell lines. Sodium ranelate did not stimulate the IP response in CHO(CaSR) cells. The IP response resulting from activation of other G-protein-coupled receptors was potentiated by Sr
2+, suggesting that entry of Sr
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2+ was comparable to that observed for Ca
2+ for both the cloned rat CaSR expressed in Chinese hamster ovary [CHO(CaSR)] cells and the mouse CaSR constitutively expressed in AtT-20 cells as measured by the accumulation of [
3H]inositol phosphates (IP) resulting from CaSR activation. Strontium ranelate also displayed comparable agonist activity for the CaSR in both cell lines. Sodium ranelate did not stimulate the IP response in CHO(CaSR) cells. The IP response resulting from activation of other G-protein-coupled receptors was potentiated by Sr
2+, suggesting that entry of Sr
2+ into the cells might influence phospholipase C activity. Modulation of the CaSR activity in bone cells by strontium ranelate may contribute to its reported antiosteoporotic effects.</description><subject>Animals</subject><subject>Calcimimetic</subject><subject>Calcium</subject><subject>Calcium - metabolism</subject><subject>CHO Cells</subject><subject>Cricetinae</subject><subject>Cricetulus</subject><subject>Divalent cations</subject><subject>Dose-Response Relationship, Drug</subject><subject>G-protein-coupled receptor</subject><subject>Life Sciences</subject><subject>Mice</subject><subject>Neurons and Cognition</subject><subject>Organometallic Compounds</subject><subject>Organometallic Compounds - pharmacology</subject><subject>Parathyroid hormone</subject><subject>Rats</subject><subject>Receptors, Calcium-Sensing</subject><subject>Receptors, Calcium-Sensing - drug effects</subject><subject>Receptors, Calcium-Sensing - physiology</subject><subject>Thiophenes</subject><subject>Thiophenes - pharmacology</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkUGLFDEQhYO4uOPqH_AgOQkeeraSTmcS8LIs6i4M7GUFbyGdVLsZejpjkh7032-aGfSmp0eFrx559Qh5x2DNgMnr3brvk1tzALEGVVW_ICsGGhrOQLwkKwCQDdfs-yV5nfMOgDEh9StyyTrRMcHZijzeT_QYSooUhwFdyTQONNd5KmHe02QnHG1BGidanpDir5Ksw3GcR5uos6OrVJNxymH6QRM6PJSY3pCLwY4Z3571inz78vnx9q7ZPny9v73ZNk6otjQ9uo53XjmmrHUKLJeihd7ZrhdCe8udBy3Btg42yimhQLYACq3y3rfWt1fk48n3yY7mkMLept8m2mDubrZmeauJpd4IfmSV_XBiDyn-nDEXsw95SVITxjkbKTVrmez-C7IN14orXkF-Al2KOScc_nyBgVkKMjuzFGSWggyoqrouvT-7z_0e_d-VcyMV-HQCsB7uGDCZ7AJODn2o5y3Gx_Av_2eAVKGn</recordid><startdate>20041029</startdate><enddate>20041029</enddate><creator>Coulombe, Josée</creator><creator>Faure, Hélène</creator><creator>Robin, Bruno</creator><creator>Ruat, Martial</creator><general>Elsevier Inc</general><general>Elsevier</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>7QP</scope><scope>7X8</scope><scope>1XC</scope></search><sort><creationdate>20041029</creationdate><title>In vitro effects of strontium ranelate on the extracellular calcium-sensing receptor</title><author>Coulombe, Josée ; Faure, Hélène ; Robin, Bruno ; Ruat, Martial</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c483t-bec525d8c18aac80a26430bca5b449da2cd0960a3c078c848063008ea8ddd3ad3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>Calcimimetic</topic><topic>Calcium</topic><topic>Calcium - metabolism</topic><topic>CHO Cells</topic><topic>Cricetinae</topic><topic>Cricetulus</topic><topic>Divalent cations</topic><topic>Dose-Response Relationship, Drug</topic><topic>G-protein-coupled receptor</topic><topic>Life Sciences</topic><topic>Mice</topic><topic>Neurons and Cognition</topic><topic>Organometallic Compounds</topic><topic>Organometallic Compounds - pharmacology</topic><topic>Parathyroid hormone</topic><topic>Rats</topic><topic>Receptors, Calcium-Sensing</topic><topic>Receptors, Calcium-Sensing - drug effects</topic><topic>Receptors, Calcium-Sensing - physiology</topic><topic>Thiophenes</topic><topic>Thiophenes - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Coulombe, Josée</creatorcontrib><creatorcontrib>Faure, Hélène</creatorcontrib><creatorcontrib>Robin, Bruno</creatorcontrib><creatorcontrib>Ruat, Martial</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><jtitle>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Coulombe, Josée</au><au>Faure, Hélène</au><au>Robin, Bruno</au><au>Ruat, Martial</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In vitro effects of strontium ranelate on the extracellular calcium-sensing receptor</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>2004-10-29</date><risdate>2004</risdate><volume>323</volume><issue>4</issue><spage>1184</spage><epage>1190</epage><pages>1184-1190</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>The extracellular calcium-sensing receptor (CaSR) is activated by divalent cations and might mediate some of the effects of strontium ranelate, a new drug for the prevention and treatment of post-menopausal osteoporosis. Here, we showed that the maximal effect of Sr
2+ was comparable to that observed for Ca
2+ for both the cloned rat CaSR expressed in Chinese hamster ovary [CHO(CaSR)] cells and the mouse CaSR constitutively expressed in AtT-20 cells as measured by the accumulation of [
3H]inositol phosphates (IP) resulting from CaSR activation. Strontium ranelate also displayed comparable agonist activity for the CaSR in both cell lines. Sodium ranelate did not stimulate the IP response in CHO(CaSR) cells. The IP response resulting from activation of other G-protein-coupled receptors was potentiated by Sr
2+, suggesting that entry of Sr
2+ into the cells might influence phospholipase C activity. Modulation of the CaSR activity in bone cells by strontium ranelate may contribute to its reported antiosteoporotic effects.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>15451421</pmid><doi>10.1016/j.bbrc.2004.08.209</doi><tpages>7</tpages></addata></record> |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Calcimimetic Calcium Calcium - metabolism CHO Cells Cricetinae Cricetulus Divalent cations Dose-Response Relationship, Drug G-protein-coupled receptor Life Sciences Mice Neurons and Cognition Organometallic Compounds Organometallic Compounds - pharmacology Parathyroid hormone Rats Receptors, Calcium-Sensing Receptors, Calcium-Sensing - drug effects Receptors, Calcium-Sensing - physiology Thiophenes Thiophenes - pharmacology |
| title | In vitro effects of strontium ranelate on the extracellular calcium-sensing receptor |
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