Prostaglandin-stimulated adenylyl cyclase activity via a pharmacologically defined EP2 receptor in human nonpigmented ciliary epithelial cells
The goal of these studies was to compare the effects of several prostaglandin (PG) receptor agonists on adenylyl cyclase activity in transformed human nonpigmented ciliary epithelial (NPE) cells. In order to define the pharmacology of the PG receptors present on these cells, cyclic AMP production wa...
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| Veröffentlicht in: | Journal of ocular pharmacology and therapeutics 1998-08, Vol.14 (4), p.293-304 |
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| creator | CRIDER, J. Y GRIFFIN, B. W SHARIF, N. A |
| description | The goal of these studies was to compare the effects of several prostaglandin (PG) receptor agonists on adenylyl cyclase activity in transformed human nonpigmented ciliary epithelial (NPE) cells. In order to define the pharmacology of the PG receptors present on these cells, cyclic AMP production was measured by both manual and robotic radioimmunoassay (RIA) techniques. In NPE cells, the rank order of potency for the PGs tested in the current study (n = up to 46) was PGE2 (EC50 = 67 nM) > 13,14-dihydro-PGE1 (EC50 = 231 nM) > 11-deoxy-PGE1 (EC50 = 500 nM) = 16,16-dimethyl-PGE2 (EC50 = 872 nM) = 11-deoxy-16,16-dimethyl-PGE2 (EC50 = 1135 nM) >> PGF2 alpha (EC50 > 10,000 nM) = PGD2 (EC50 > 10,000 nM) = PGI2 (EC50 > 10,000 nM). The EP2-receptor selective PG, butaprost, exhibited a potency of 212 nM (Emax = 55%). The response to 1 microM PGE2 was antagonized by AH6809 (IC50 = approximately 50 microM, Kb = 4 microM). The relative potencies of the EP agonists mentioned above were significantly weaker in EbTr and NCB-20 cells expressing DP and IP receptors, respectively (1). These data provide a detailed pharmacological identification and characterization of EP2 receptors on NPE cells. |
| doi_str_mv | 10.1089/jop.1998.14.293 |
| format | Article |
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Y ; GRIFFIN, B. W ; SHARIF, N. A</creator><creatorcontrib>CRIDER, J. Y ; GRIFFIN, B. W ; SHARIF, N. A</creatorcontrib><description>The goal of these studies was to compare the effects of several prostaglandin (PG) receptor agonists on adenylyl cyclase activity in transformed human nonpigmented ciliary epithelial (NPE) cells. In order to define the pharmacology of the PG receptors present on these cells, cyclic AMP production was measured by both manual and robotic radioimmunoassay (RIA) techniques. In NPE cells, the rank order of potency for the PGs tested in the current study (n = up to 46) was PGE2 (EC50 = 67 nM) > 13,14-dihydro-PGE1 (EC50 = 231 nM) > 11-deoxy-PGE1 (EC50 = 500 nM) = 16,16-dimethyl-PGE2 (EC50 = 872 nM) = 11-deoxy-16,16-dimethyl-PGE2 (EC50 = 1135 nM) >> PGF2 alpha (EC50 > 10,000 nM) = PGD2 (EC50 > 10,000 nM) = PGI2 (EC50 > 10,000 nM). The EP2-receptor selective PG, butaprost, exhibited a potency of 212 nM (Emax = 55%). The response to 1 microM PGE2 was antagonized by AH6809 (IC50 = approximately 50 microM, Kb = 4 microM). The relative potencies of the EP agonists mentioned above were significantly weaker in EbTr and NCB-20 cells expressing DP and IP receptors, respectively (1). These data provide a detailed pharmacological identification and characterization of EP2 receptors on NPE cells.</description><identifier>ISSN: 1080-7683</identifier><identifier>EISSN: 1557-7732</identifier><identifier>DOI: 10.1089/jop.1998.14.293</identifier><identifier>PMID: 9715432</identifier><language>eng</language><publisher>Larchmont, NY: Liebert</publisher><subject>Adenylyl Cyclases - metabolism ; Biological and medical sciences ; Cell Line, Transformed ; Cells, Cultured ; Ciliary Body - drug effects ; Ciliary Body - enzymology ; Cyclic AMP - metabolism ; Epithelial Cells - drug effects ; Epithelial Cells - enzymology ; Fundamental and applied biological sciences. Psychology ; Humans ; Prostaglandins - pharmacology ; Radioimmunoassay ; Receptors, Prostaglandin E - metabolism ; Receptors, Prostaglandin E, EP2 Subtype ; Vertebrates: skin, associated glands, phaneres, light organs, various exocrine glands (salt gland, uropygial gland...), adipose tissue, connective tissue</subject><ispartof>Journal of ocular pharmacology and therapeutics, 1998-08, Vol.14 (4), p.293-304</ispartof><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>309,310,314,780,784,789,790,23930,23931,25140,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1605691$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9715432$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>CRIDER, J. Y</creatorcontrib><creatorcontrib>GRIFFIN, B. W</creatorcontrib><creatorcontrib>SHARIF, N. A</creatorcontrib><title>Prostaglandin-stimulated adenylyl cyclase activity via a pharmacologically defined EP2 receptor in human nonpigmented ciliary epithelial cells</title><title>Journal of ocular pharmacology and therapeutics</title><addtitle>J Ocul Pharmacol Ther</addtitle><description>The goal of these studies was to compare the effects of several prostaglandin (PG) receptor agonists on adenylyl cyclase activity in transformed human nonpigmented ciliary epithelial (NPE) cells. In order to define the pharmacology of the PG receptors present on these cells, cyclic AMP production was measured by both manual and robotic radioimmunoassay (RIA) techniques. In NPE cells, the rank order of potency for the PGs tested in the current study (n = up to 46) was PGE2 (EC50 = 67 nM) > 13,14-dihydro-PGE1 (EC50 = 231 nM) > 11-deoxy-PGE1 (EC50 = 500 nM) = 16,16-dimethyl-PGE2 (EC50 = 872 nM) = 11-deoxy-16,16-dimethyl-PGE2 (EC50 = 1135 nM) >> PGF2 alpha (EC50 > 10,000 nM) = PGD2 (EC50 > 10,000 nM) = PGI2 (EC50 > 10,000 nM). The EP2-receptor selective PG, butaprost, exhibited a potency of 212 nM (Emax = 55%). The response to 1 microM PGE2 was antagonized by AH6809 (IC50 = approximately 50 microM, Kb = 4 microM). The relative potencies of the EP agonists mentioned above were significantly weaker in EbTr and NCB-20 cells expressing DP and IP receptors, respectively (1). These data provide a detailed pharmacological identification and characterization of EP2 receptors on NPE cells.</description><subject>Adenylyl Cyclases - metabolism</subject><subject>Biological and medical sciences</subject><subject>Cell Line, Transformed</subject><subject>Cells, Cultured</subject><subject>Ciliary Body - drug effects</subject><subject>Ciliary Body - enzymology</subject><subject>Cyclic AMP - metabolism</subject><subject>Epithelial Cells - drug effects</subject><subject>Epithelial Cells - enzymology</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Humans</subject><subject>Prostaglandins - pharmacology</subject><subject>Radioimmunoassay</subject><subject>Receptors, Prostaglandin E - metabolism</subject><subject>Receptors, Prostaglandin E, EP2 Subtype</subject><subject>Vertebrates: skin, associated glands, phaneres, light organs, various exocrine glands (salt gland, uropygial gland...), adipose tissue, connective tissue</subject><issn>1080-7683</issn><issn>1557-7732</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9UMtKxDAUDaKMz7UrIQtx15pH06RLGcYHDOhC18Ntks5E0rQ26UB_wm-24uDqHjiPezgIXVOSU6Kq-8-uz2lVqZwWOav4ETqjQshMSs6OZ0wUyWSp-Ck6j_GTEMpJSRdoUUkqCs7O0Pfb0MUEWw_BuJDF5NrRQ7IGg7Fh8pPHetIeosWgk9u7NOG9Awy438HQgu58t3UavJ-wsY0Ls3P1xvBgte1TN2AX8G5sIeDQhd5tWxt-w7XzDoYJ296lnZ3x_MZ6Hy_RSQM-2qvDvUAfj6v35XO2fn16WT6ss55xkTIJsjBKGKNr0wiiNRc1LVUhSAOi5lxYQgiTjJgaWGGEMrwgolZgeGm1avgFuvvL7Yfua7QxbVoXfxtAsN0YN5IrwVRBZ-HNQTjWrTWbfnDtXHxzGHDmbw88xHmFZoCgXfyX0ZKIsqL8BxGFg20</recordid><startdate>19980801</startdate><enddate>19980801</enddate><creator>CRIDER, J. Y</creator><creator>GRIFFIN, B. W</creator><creator>SHARIF, N. A</creator><general>Liebert</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>19980801</creationdate><title>Prostaglandin-stimulated adenylyl cyclase activity via a pharmacologically defined EP2 receptor in human nonpigmented ciliary epithelial cells</title><author>CRIDER, J. Y ; GRIFFIN, B. W ; SHARIF, N. A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p235t-7a74d85ddcbdf50cc35b168450fa5b335e0002720dba24d58d3405b8ad36ec8f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Adenylyl Cyclases - metabolism</topic><topic>Biological and medical sciences</topic><topic>Cell Line, Transformed</topic><topic>Cells, Cultured</topic><topic>Ciliary Body - drug effects</topic><topic>Ciliary Body - enzymology</topic><topic>Cyclic AMP - metabolism</topic><topic>Epithelial Cells - drug effects</topic><topic>Epithelial Cells - enzymology</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Humans</topic><topic>Prostaglandins - pharmacology</topic><topic>Radioimmunoassay</topic><topic>Receptors, Prostaglandin E - metabolism</topic><topic>Receptors, Prostaglandin E, EP2 Subtype</topic><topic>Vertebrates: skin, associated glands, phaneres, light organs, various exocrine glands (salt gland, uropygial gland...), adipose tissue, connective tissue</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>CRIDER, J. Y</creatorcontrib><creatorcontrib>GRIFFIN, B. W</creatorcontrib><creatorcontrib>SHARIF, N. A</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>MEDLINE - Academic</collection><jtitle>Journal of ocular pharmacology and therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>CRIDER, J. Y</au><au>GRIFFIN, B. W</au><au>SHARIF, N. A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Prostaglandin-stimulated adenylyl cyclase activity via a pharmacologically defined EP2 receptor in human nonpigmented ciliary epithelial cells</atitle><jtitle>Journal of ocular pharmacology and therapeutics</jtitle><addtitle>J Ocul Pharmacol Ther</addtitle><date>1998-08-01</date><risdate>1998</risdate><volume>14</volume><issue>4</issue><spage>293</spage><epage>304</epage><pages>293-304</pages><issn>1080-7683</issn><eissn>1557-7732</eissn><abstract>The goal of these studies was to compare the effects of several prostaglandin (PG) receptor agonists on adenylyl cyclase activity in transformed human nonpigmented ciliary epithelial (NPE) cells. In order to define the pharmacology of the PG receptors present on these cells, cyclic AMP production was measured by both manual and robotic radioimmunoassay (RIA) techniques. In NPE cells, the rank order of potency for the PGs tested in the current study (n = up to 46) was PGE2 (EC50 = 67 nM) > 13,14-dihydro-PGE1 (EC50 = 231 nM) > 11-deoxy-PGE1 (EC50 = 500 nM) = 16,16-dimethyl-PGE2 (EC50 = 872 nM) = 11-deoxy-16,16-dimethyl-PGE2 (EC50 = 1135 nM) >> PGF2 alpha (EC50 > 10,000 nM) = PGD2 (EC50 > 10,000 nM) = PGI2 (EC50 > 10,000 nM). The EP2-receptor selective PG, butaprost, exhibited a potency of 212 nM (Emax = 55%). The response to 1 microM PGE2 was antagonized by AH6809 (IC50 = approximately 50 microM, Kb = 4 microM). The relative potencies of the EP agonists mentioned above were significantly weaker in EbTr and NCB-20 cells expressing DP and IP receptors, respectively (1). These data provide a detailed pharmacological identification and characterization of EP2 receptors on NPE cells.</abstract><cop>Larchmont, NY</cop><pub>Liebert</pub><pmid>9715432</pmid><doi>10.1089/jop.1998.14.293</doi><tpages>12</tpages></addata></record> |
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| subjects | Adenylyl Cyclases - metabolism Biological and medical sciences Cell Line, Transformed Cells, Cultured Ciliary Body - drug effects Ciliary Body - enzymology Cyclic AMP - metabolism Epithelial Cells - drug effects Epithelial Cells - enzymology Fundamental and applied biological sciences. Psychology Humans Prostaglandins - pharmacology Radioimmunoassay Receptors, Prostaglandin E - metabolism Receptors, Prostaglandin E, EP2 Subtype Vertebrates: skin, associated glands, phaneres, light organs, various exocrine glands (salt gland, uropygial gland...), adipose tissue, connective tissue |
| title | Prostaglandin-stimulated adenylyl cyclase activity via a pharmacologically defined EP2 receptor in human nonpigmented ciliary epithelial cells |
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