Effects of anandamide on cannabinoid receptors in rat brain membranes
Anandamide (arachidonylethanolamide) is a compound recently isolated from porcine brain as a putative endogenous ligand at cannabinoid receptors. The present studies examined the effects of anandamide on cannabinoid receptor binding sites and adenylyl cyclase in rat brain membranes. Receptor binding...
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| Veröffentlicht in: | Biochemical pharmacology 1994-02, Vol.47 (4), p.711-715 |
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| container_title | Biochemical pharmacology |
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| creator | Childers, Steven R. Sexton, Tammy Roy, Mary Beth |
| description | Anandamide (arachidonylethanolamide) is a compound recently isolated from porcine brain as a putative endogenous ligand at cannabinoid receptors. The present studies examined the effects of anandamide on cannabinoid receptor binding sites and adenylyl cyclase in rat brain membranes. Receptor binding experiments, conducted at 25° for 90 min, apparently resulted in significant degradation of anandamide, since anandamide (10 μM) had little effect on [
3H]WIN 55212-2 binding in cerebellar membranes. Addition of the general serine protease inhibitor phenylmethylsulfonyl fluoride (PMSF) protected against this degradation, resulting in an
ic
50 value of 90 nM for anandamide versus [
4H]WIN 55212-2 binding. Anandamide inhibited adenylyl cyclase in cerebellar membranes in a GTP-dependent manner, exhibiting a maximal inhibition level slightly less than that of WIN 55212-2 and CP-55,940, with an
ic
50 value of 1.9 μM. The effect of anandamide on adenylyl cyclase was region-specific, with maximal inhibition occurring in cerebellum and striatum. These results suggest that anandamide acts at G-protein-coupled cannabinoid receptors in brain with properties similar to those of exogenous cannabinoids. |
| doi_str_mv | 10.1016/0006-2952(94)90134-1 |
| format | Article |
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3H]WIN 55212-2 binding in cerebellar membranes. Addition of the general serine protease inhibitor phenylmethylsulfonyl fluoride (PMSF) protected against this degradation, resulting in an
ic
50 value of 90 nM for anandamide versus [
4H]WIN 55212-2 binding. Anandamide inhibited adenylyl cyclase in cerebellar membranes in a GTP-dependent manner, exhibiting a maximal inhibition level slightly less than that of WIN 55212-2 and CP-55,940, with an
ic
50 value of 1.9 μM. The effect of anandamide on adenylyl cyclase was region-specific, with maximal inhibition occurring in cerebellum and striatum. These results suggest that anandamide acts at G-protein-coupled cannabinoid receptors in brain with properties similar to those of exogenous cannabinoids.</description><identifier>ISSN: 0006-2952</identifier><identifier>EISSN: 1873-2968</identifier><identifier>DOI: 10.1016/0006-2952(94)90134-1</identifier><identifier>PMID: 8129747</identifier><language>eng</language><publisher>England: Elsevier Inc</publisher><subject>adenylyl cyclase ; Adenylyl Cyclase Inhibitors ; Amides - pharmacology ; Amidohydrolases - antagonists & inhibitors ; Animals ; Arachidonic Acids ; arachidonylethanolamide ; Benzoxazines ; Binding, Competitive ; Brain Chemistry ; Dose-Response Relationship, Drug ; Endocannabinoids ; Fatty Acids, Unsaturated - pharmacology ; GTP-Binding Proteins - metabolism ; Morpholines - pharmacology ; Naphthalenes - pharmacology ; phenylmethylsulfonyl fluoride ; Phenylmethylsulfonyl Fluoride - pharmacology ; Polyunsaturated Alkamides ; Rats ; Receptors, Cannabinoid ; Receptors, Drug - drug effects ; Δ-tetrahydrocannibinol</subject><ispartof>Biochemical pharmacology, 1994-02, Vol.47 (4), p.711-715</ispartof><rights>1994</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c388t-58bbdf0d15f52da30bc395d1b9851536c66014fa0ae415f649bba673c98c3ccb3</citedby><cites>FETCH-LOGICAL-c388t-58bbdf0d15f52da30bc395d1b9851536c66014fa0ae415f649bba673c98c3ccb3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0006-2952(94)90134-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27926,27927,45997</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8129747$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Childers, Steven R.</creatorcontrib><creatorcontrib>Sexton, Tammy</creatorcontrib><creatorcontrib>Roy, Mary Beth</creatorcontrib><title>Effects of anandamide on cannabinoid receptors in rat brain membranes</title><title>Biochemical pharmacology</title><addtitle>Biochem Pharmacol</addtitle><description>Anandamide (arachidonylethanolamide) is a compound recently isolated from porcine brain as a putative endogenous ligand at cannabinoid receptors. The present studies examined the effects of anandamide on cannabinoid receptor binding sites and adenylyl cyclase in rat brain membranes. Receptor binding experiments, conducted at 25° for 90 min, apparently resulted in significant degradation of anandamide, since anandamide (10 μM) had little effect on [
3H]WIN 55212-2 binding in cerebellar membranes. Addition of the general serine protease inhibitor phenylmethylsulfonyl fluoride (PMSF) protected against this degradation, resulting in an
ic
50 value of 90 nM for anandamide versus [
4H]WIN 55212-2 binding. Anandamide inhibited adenylyl cyclase in cerebellar membranes in a GTP-dependent manner, exhibiting a maximal inhibition level slightly less than that of WIN 55212-2 and CP-55,940, with an
ic
50 value of 1.9 μM. The effect of anandamide on adenylyl cyclase was region-specific, with maximal inhibition occurring in cerebellum and striatum. These results suggest that anandamide acts at G-protein-coupled cannabinoid receptors in brain with properties similar to those of exogenous cannabinoids.</description><subject>adenylyl cyclase</subject><subject>Adenylyl Cyclase Inhibitors</subject><subject>Amides - pharmacology</subject><subject>Amidohydrolases - antagonists & inhibitors</subject><subject>Animals</subject><subject>Arachidonic Acids</subject><subject>arachidonylethanolamide</subject><subject>Benzoxazines</subject><subject>Binding, Competitive</subject><subject>Brain Chemistry</subject><subject>Dose-Response Relationship, Drug</subject><subject>Endocannabinoids</subject><subject>Fatty Acids, Unsaturated - pharmacology</subject><subject>GTP-Binding Proteins - metabolism</subject><subject>Morpholines - pharmacology</subject><subject>Naphthalenes - pharmacology</subject><subject>phenylmethylsulfonyl fluoride</subject><subject>Phenylmethylsulfonyl Fluoride - pharmacology</subject><subject>Polyunsaturated Alkamides</subject><subject>Rats</subject><subject>Receptors, Cannabinoid</subject><subject>Receptors, Drug - drug effects</subject><subject>Δ-tetrahydrocannibinol</subject><issn>0006-2952</issn><issn>1873-2968</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtKAzEUhoMotVbfQCEr0cVo0mQyyUaQUi9QcKPrkCtEOklNpoJvb8aWLl2d239uHwCXGN1hhNk9Qog1c9HObwS9FQgT2uAjMMW8IzXN-DGYHiSn4KyUzzHkDE_AhOO56Gg3Bcul984MBSYPVVTRqj5YB1OERsWodIgpWJidcZsh5QJDhFkNUGdVvd711YmunIMTr9bFXeztDHw8Ld8XL83q7fl18bhqDOF8aFqutfXI4ta3c6sI0oaI1mIteItbwgxjCFOvkHK0ahgVWivWESO4IcZoMgPXu7mbnL62rgyyD8W49boekbZFYsYRQQJXId0JTU6lZOflJode5R-JkRzpyZGFHNFIQeUfPTm2Xe3nb3Xv7KFpj6vWH3Z1V5_8Di7LYoKLxtlQEQ3SpvD_gl-oEH4b</recordid><startdate>19940211</startdate><enddate>19940211</enddate><creator>Childers, Steven R.</creator><creator>Sexton, Tammy</creator><creator>Roy, Mary Beth</creator><general>Elsevier Inc</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>7TK</scope></search><sort><creationdate>19940211</creationdate><title>Effects of anandamide on cannabinoid receptors in rat brain membranes</title><author>Childers, Steven R. ; Sexton, Tammy ; Roy, Mary Beth</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c388t-58bbdf0d15f52da30bc395d1b9851536c66014fa0ae415f649bba673c98c3ccb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>adenylyl cyclase</topic><topic>Adenylyl Cyclase Inhibitors</topic><topic>Amides - pharmacology</topic><topic>Amidohydrolases - antagonists & inhibitors</topic><topic>Animals</topic><topic>Arachidonic Acids</topic><topic>arachidonylethanolamide</topic><topic>Benzoxazines</topic><topic>Binding, Competitive</topic><topic>Brain Chemistry</topic><topic>Dose-Response Relationship, Drug</topic><topic>Endocannabinoids</topic><topic>Fatty Acids, Unsaturated - pharmacology</topic><topic>GTP-Binding Proteins - metabolism</topic><topic>Morpholines - pharmacology</topic><topic>Naphthalenes - pharmacology</topic><topic>phenylmethylsulfonyl fluoride</topic><topic>Phenylmethylsulfonyl Fluoride - pharmacology</topic><topic>Polyunsaturated Alkamides</topic><topic>Rats</topic><topic>Receptors, Cannabinoid</topic><topic>Receptors, Drug - drug effects</topic><topic>Δ-tetrahydrocannibinol</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Childers, Steven R.</creatorcontrib><creatorcontrib>Sexton, Tammy</creatorcontrib><creatorcontrib>Roy, Mary Beth</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><jtitle>Biochemical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Childers, Steven R.</au><au>Sexton, Tammy</au><au>Roy, Mary Beth</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of anandamide on cannabinoid receptors in rat brain membranes</atitle><jtitle>Biochemical pharmacology</jtitle><addtitle>Biochem Pharmacol</addtitle><date>1994-02-11</date><risdate>1994</risdate><volume>47</volume><issue>4</issue><spage>711</spage><epage>715</epage><pages>711-715</pages><issn>0006-2952</issn><eissn>1873-2968</eissn><abstract>Anandamide (arachidonylethanolamide) is a compound recently isolated from porcine brain as a putative endogenous ligand at cannabinoid receptors. The present studies examined the effects of anandamide on cannabinoid receptor binding sites and adenylyl cyclase in rat brain membranes. Receptor binding experiments, conducted at 25° for 90 min, apparently resulted in significant degradation of anandamide, since anandamide (10 μM) had little effect on [
3H]WIN 55212-2 binding in cerebellar membranes. Addition of the general serine protease inhibitor phenylmethylsulfonyl fluoride (PMSF) protected against this degradation, resulting in an
ic
50 value of 90 nM for anandamide versus [
4H]WIN 55212-2 binding. Anandamide inhibited adenylyl cyclase in cerebellar membranes in a GTP-dependent manner, exhibiting a maximal inhibition level slightly less than that of WIN 55212-2 and CP-55,940, with an
ic
50 value of 1.9 μM. The effect of anandamide on adenylyl cyclase was region-specific, with maximal inhibition occurring in cerebellum and striatum. These results suggest that anandamide acts at G-protein-coupled cannabinoid receptors in brain with properties similar to those of exogenous cannabinoids.</abstract><cop>England</cop><pub>Elsevier Inc</pub><pmid>8129747</pmid><doi>10.1016/0006-2952(94)90134-1</doi><tpages>5</tpages></addata></record> |
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| ispartof | Biochemical pharmacology, 1994-02, Vol.47 (4), p.711-715 |
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| subjects | adenylyl cyclase Adenylyl Cyclase Inhibitors Amides - pharmacology Amidohydrolases - antagonists & inhibitors Animals Arachidonic Acids arachidonylethanolamide Benzoxazines Binding, Competitive Brain Chemistry Dose-Response Relationship, Drug Endocannabinoids Fatty Acids, Unsaturated - pharmacology GTP-Binding Proteins - metabolism Morpholines - pharmacology Naphthalenes - pharmacology phenylmethylsulfonyl fluoride Phenylmethylsulfonyl Fluoride - pharmacology Polyunsaturated Alkamides Rats Receptors, Cannabinoid Receptors, Drug - drug effects Δ-tetrahydrocannibinol |
| title | Effects of anandamide on cannabinoid receptors in rat brain membranes |
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