The enigmatic pharmacology of GPR55
Preliminary data presented at conferences and in the patent literature introduced the possibility the orphan receptor GPR55 might account for some of the well-documented non-CB1 , non-CB2 effects reported for certain cannabinoid ligands. Several peer-reviewed publications have recently emerged in wh...
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Veröffentlicht in: | Trends in pharmacological sciences (Regular ed.) 2009-03, Vol.30 (3), p.156-163 |
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description | Preliminary data presented at conferences and in the patent literature introduced the possibility the orphan receptor GPR55 might account for some of the well-documented non-CB1 , non-CB2 effects reported for certain cannabinoid ligands. Several peer-reviewed publications have recently emerged in which the pharmacology of the cannabinoids at GPR55 has been probed in more depth. Despite this, the classification of GPR55 as a cannabinoid receptor remains a contentious issue. The weight of evidence points to GPR55 as a receptor that is activated by certain cannabinoid ligands and by the bioactive lipid l -α-lysophosphatidylinsoitol. It couples to G12 proteins, activates RhoA and mobilizes intracellular Ca2+ , possibly in an agonist- and tissue-dependant manner, thus displaying ‘agonist functional selectivity’. Here, I review the recent literature in an effort to glean the key controversies and outstanding questions surrounding the interaction between cannabinoids and this orphan receptor. |
doi_str_mv | 10.1016/j.tips.2008.12.004 |
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Several peer-reviewed publications have recently emerged in which the pharmacology of the cannabinoids at GPR55 has been probed in more depth. Despite this, the classification of GPR55 as a cannabinoid receptor remains a contentious issue. The weight of evidence points to GPR55 as a receptor that is activated by certain cannabinoid ligands and by the bioactive lipid l -α-lysophosphatidylinsoitol. It couples to G12 proteins, activates RhoA and mobilizes intracellular Ca2+ , possibly in an agonist- and tissue-dependant manner, thus displaying ‘agonist functional selectivity’. Here, I review the recent literature in an effort to glean the key controversies and outstanding questions surrounding the interaction between cannabinoids and this orphan receptor.</description><identifier>ISSN: 0165-6147</identifier><identifier>EISSN: 1873-3735</identifier><identifier>DOI: 10.1016/j.tips.2008.12.004</identifier><identifier>PMID: 19233486</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Advanced Basic Science ; Animals ; Binding Sites ; Cannabinoid Receptor Agonists ; Cannabinoid Receptor Modulators - metabolism ; Cannabinoid Receptor Modulators - pharmacology ; Cannabinoids - metabolism ; Cannabinoids - pharmacology ; Ligands ; Lysophospholipids - metabolism ; Lysophospholipids - pharmacology ; Mice ; Receptors, Cannabinoid - classification ; Receptors, Cannabinoid - physiology ; Receptors, Lysophospholipid - agonists ; Receptors, Lysophospholipid - classification ; Receptors, Lysophospholipid - physiology ; Signal Transduction - drug effects ; Structure-Activity Relationship</subject><ispartof>Trends in pharmacological sciences (Regular ed.), 2009-03, Vol.30 (3), p.156-163</ispartof><rights>Elsevier Ltd</rights><rights>2008 Elsevier Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c409t-f507534b59b6e2a1028bdb9964182672cebe4eb32ec3dfd02d70eda7f7e795b83</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0165614709000170$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19233486$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ross, Ruth A</creatorcontrib><title>The enigmatic pharmacology of GPR55</title><title>Trends in pharmacological sciences (Regular ed.)</title><addtitle>Trends Pharmacol Sci</addtitle><description>Preliminary data presented at conferences and in the patent literature introduced the possibility the orphan receptor GPR55 might account for some of the well-documented non-CB1 , non-CB2 effects reported for certain cannabinoid ligands. 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Here, I review the recent literature in an effort to glean the key controversies and outstanding questions surrounding the interaction between cannabinoids and this orphan receptor.</description><subject>Advanced Basic Science</subject><subject>Animals</subject><subject>Binding Sites</subject><subject>Cannabinoid Receptor Agonists</subject><subject>Cannabinoid Receptor Modulators - metabolism</subject><subject>Cannabinoid Receptor Modulators - pharmacology</subject><subject>Cannabinoids - metabolism</subject><subject>Cannabinoids - pharmacology</subject><subject>Ligands</subject><subject>Lysophospholipids - metabolism</subject><subject>Lysophospholipids - pharmacology</subject><subject>Mice</subject><subject>Receptors, Cannabinoid - classification</subject><subject>Receptors, Cannabinoid - physiology</subject><subject>Receptors, Lysophospholipid - agonists</subject><subject>Receptors, Lysophospholipid - classification</subject><subject>Receptors, Lysophospholipid - physiology</subject><subject>Signal Transduction - drug effects</subject><subject>Structure-Activity Relationship</subject><issn>0165-6147</issn><issn>1873-3735</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kV1LwzAUhoMobn78AS9kIHjXepK0TQsiyNApDBSd1yFNT7fMfsykFfbvTdlA8MKrc_O8L5znJeSCQkiBJjfrsDMbFzKANKQsBIgOyJimggdc8PiQjD0UBwmNxIicOLcGAM4ZPSYjmjHOozQZk6vFCifYmGWtOqMnm5WytdJt1S63k7aczF7f4viMHJWqcni-v6fk4_FhMX0K5i-z5-n9PNARZF1QxiBiHuVxlifIFAWW5kWeZUlEU5YIpjHHCHPOUPOiLIAVArBQohQosjhP-Sm53vVubPvVo-tkbZzGqlINtr2TiQDIEs48yHagtq1zFku5saZWdispyEGNXMtBjRzUSMqkV-NDl_v2Pq-x-I3sXXjgdgeg__HboJVOG2w0Fsai7mTRmv_77_7EdWUao1X1iVt067a3jbcnqXQ-IN-HcYZtIPO7UAH8B260h-E</recordid><startdate>20090301</startdate><enddate>20090301</enddate><creator>Ross, Ruth A</creator><general>Elsevier Ltd</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>7X8</scope></search><sort><creationdate>20090301</creationdate><title>The enigmatic pharmacology of GPR55</title><author>Ross, Ruth A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c409t-f507534b59b6e2a1028bdb9964182672cebe4eb32ec3dfd02d70eda7f7e795b83</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Advanced Basic Science</topic><topic>Animals</topic><topic>Binding Sites</topic><topic>Cannabinoid Receptor Agonists</topic><topic>Cannabinoid Receptor Modulators - metabolism</topic><topic>Cannabinoid Receptor Modulators - pharmacology</topic><topic>Cannabinoids - metabolism</topic><topic>Cannabinoids - pharmacology</topic><topic>Ligands</topic><topic>Lysophospholipids - metabolism</topic><topic>Lysophospholipids - pharmacology</topic><topic>Mice</topic><topic>Receptors, Cannabinoid - classification</topic><topic>Receptors, Cannabinoid - physiology</topic><topic>Receptors, Lysophospholipid - agonists</topic><topic>Receptors, Lysophospholipid - classification</topic><topic>Receptors, Lysophospholipid - physiology</topic><topic>Signal Transduction - drug effects</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ross, Ruth A</creatorcontrib><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>Trends in pharmacological sciences (Regular ed.)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ross, Ruth A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The enigmatic pharmacology of GPR55</atitle><jtitle>Trends in pharmacological sciences (Regular ed.)</jtitle><addtitle>Trends Pharmacol Sci</addtitle><date>2009-03-01</date><risdate>2009</risdate><volume>30</volume><issue>3</issue><spage>156</spage><epage>163</epage><pages>156-163</pages><issn>0165-6147</issn><eissn>1873-3735</eissn><abstract>Preliminary data presented at conferences and in the patent literature introduced the possibility the orphan receptor GPR55 might account for some of the well-documented non-CB1 , non-CB2 effects reported for certain cannabinoid ligands. 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subjects | Advanced Basic Science Animals Binding Sites Cannabinoid Receptor Agonists Cannabinoid Receptor Modulators - metabolism Cannabinoid Receptor Modulators - pharmacology Cannabinoids - metabolism Cannabinoids - pharmacology Ligands Lysophospholipids - metabolism Lysophospholipids - pharmacology Mice Receptors, Cannabinoid - classification Receptors, Cannabinoid - physiology Receptors, Lysophospholipid - agonists Receptors, Lysophospholipid - classification Receptors, Lysophospholipid - physiology Signal Transduction - drug effects Structure-Activity Relationship |
title | The enigmatic pharmacology of GPR55 |
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