Stimulation of glycogenolysis in isolated hepatocytes by adenosine and one of its analogues is inhibited by caffeine
The adenosine analogues 5'-(N-ethyl)carboxamidoadenosine (NECA) and N6-(phenylisopropyl)adenosine (PIA) activate glycogen phosphorylase 5-fold and 4.2-fold respectively in rat hepatocytes incubated in the absence of endogenous adenosine. Half-maximally effective concentrations are 0.5 microM fo...
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| Veröffentlicht in: | Biochemical journal 1987-11, Vol.247 (3), p.779-783 |
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| container_title | Biochemical journal |
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| creator | Stanley, J.C Markovic, J Gutknecht, A.M Lozeman, F.J |
| description | The adenosine analogues 5'-(N-ethyl)carboxamidoadenosine (NECA) and N6-(phenylisopropyl)adenosine (PIA) activate glycogen phosphorylase 5-fold and 4.2-fold respectively in rat hepatocytes incubated in the absence of endogenous adenosine. Half-maximally effective concentrations are 0.5 microM for NECA and 20 microM for PIA, demonstrating the presence of A2-adenosine receptors. Exogenous adenosine activates phosphorylase 4.6-fold, but high rates of adenosine disappearance from the medium render estimates of its half-maximally effective concentration unreliable. These effects of NECA and adenosine are inhibited by 0.1 mM-caffeine. Activation of phosphorylase by a physiological concentration of adenosine (3.3 microM) was 50% inhibited by a physiological concentration of caffeine (35 microM). |
| doi_str_mv | 10.1042/bj2470779 |
| format | Article |
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Half-maximally effective concentrations are 0.5 microM for NECA and 20 microM for PIA, demonstrating the presence of A2-adenosine receptors. Exogenous adenosine activates phosphorylase 4.6-fold, but high rates of adenosine disappearance from the medium render estimates of its half-maximally effective concentration unreliable. These effects of NECA and adenosine are inhibited by 0.1 mM-caffeine. Activation of phosphorylase by a physiological concentration of adenosine (3.3 microM) was 50% inhibited by a physiological concentration of caffeine (35 microM).</description><identifier>ISSN: 0264-6021</identifier><identifier>EISSN: 1470-8728</identifier><identifier>DOI: 10.1042/bj2470779</identifier><identifier>PMID: 3426562</identifier><language>eng</language><publisher>England</publisher><subject>adenosine ; Adenosine - analogs & derivatives ; Adenosine - antagonists & inhibitors ; Adenosine - pharmacology ; Adenosine Deaminase - pharmacology ; Adenosine-5'-(N-ethylcarboxamide) ; Animals ; caffeine ; Caffeine - pharmacology ; Cell Separation ; Dose-Response Relationship, Drug ; Enzyme Activation - drug effects ; Glucagon - pharmacology ; glycogenolysis ; In Vitro Techniques ; inhibition ; liver ; Liver - drug effects ; Liver - metabolism ; Liver Glycogen - metabolism ; Male ; Phenylisopropyladenosine - pharmacology ; Phosphorylases - antagonists & inhibitors ; Rats ; Rats, Inbred Strains ; stimulation ; Stimulation, Chemical</subject><ispartof>Biochemical journal, 1987-11, Vol.247 (3), p.779-783</ispartof><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c449t-57b4eb5db4008d8b67707be1afbccc16ffe6c0bb5b135072c34a353b8d7359a33</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1148479/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1148479/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3426562$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Stanley, J.C</creatorcontrib><creatorcontrib>Markovic, J</creatorcontrib><creatorcontrib>Gutknecht, A.M</creatorcontrib><creatorcontrib>Lozeman, F.J</creatorcontrib><title>Stimulation of glycogenolysis in isolated hepatocytes by adenosine and one of its analogues is inhibited by caffeine</title><title>Biochemical journal</title><addtitle>Biochem J</addtitle><description>The adenosine analogues 5'-(N-ethyl)carboxamidoadenosine (NECA) and N6-(phenylisopropyl)adenosine (PIA) activate glycogen phosphorylase 5-fold and 4.2-fold respectively in rat hepatocytes incubated in the absence of endogenous adenosine. Half-maximally effective concentrations are 0.5 microM for NECA and 20 microM for PIA, demonstrating the presence of A2-adenosine receptors. Exogenous adenosine activates phosphorylase 4.6-fold, but high rates of adenosine disappearance from the medium render estimates of its half-maximally effective concentration unreliable. These effects of NECA and adenosine are inhibited by 0.1 mM-caffeine. Activation of phosphorylase by a physiological concentration of adenosine (3.3 microM) was 50% inhibited by a physiological concentration of caffeine (35 microM).</description><subject>adenosine</subject><subject>Adenosine - analogs & derivatives</subject><subject>Adenosine - antagonists & inhibitors</subject><subject>Adenosine - pharmacology</subject><subject>Adenosine Deaminase - pharmacology</subject><subject>Adenosine-5'-(N-ethylcarboxamide)</subject><subject>Animals</subject><subject>caffeine</subject><subject>Caffeine - pharmacology</subject><subject>Cell Separation</subject><subject>Dose-Response Relationship, Drug</subject><subject>Enzyme Activation - drug effects</subject><subject>Glucagon - pharmacology</subject><subject>glycogenolysis</subject><subject>In Vitro Techniques</subject><subject>inhibition</subject><subject>liver</subject><subject>Liver - drug effects</subject><subject>Liver - metabolism</subject><subject>Liver Glycogen - metabolism</subject><subject>Male</subject><subject>Phenylisopropyladenosine - pharmacology</subject><subject>Phosphorylases - antagonists & inhibitors</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>stimulation</subject><subject>Stimulation, Chemical</subject><issn>0264-6021</issn><issn>1470-8728</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkk1r3DAQhkVJSbZpD_0BIToVcnAz-rBkXwJh6Rcs5JDkLCRZ9ip4rY0lB_zvq80uS3pJTyPxPu_LDDMIfSXwnQCn1-aJcglS1h_QguRXUUlanaAFUMELAZScoU8xPgEQDhxO0SnjVJSCLlC6T34z9Tr5MODQ4q6fbejcEPo5-oj9gH0MWXYNXrutTsHOyUVsZqybTEU_OKyHBodcs92nmL-6D92UqdeAtTd-Z88Wq9vWZcdn9LHVfXRfDvUcPf788bD8Xazufv1Z3q4Ky3mdilIa7kzZGA5QNZURMs9oHNGtsdYSkcOEBWNKQ1gJklrGNSuZqRrJylozdo5u9rnbyWxcY92QRt2r7eg3epxV0F79qwx-rbrwogjhFZd1Dvh2CBjDc54oqY2P1vW9HlyYopKyqpkU_wcJrwWRfAde7UE7hhhH1x67IaB2u1THXWb24m37R_KwvKxf7vVWB6W70Uf1eE-BMKAgaM3hHSIfAmGMsr9riK8h</recordid><startdate>19871101</startdate><enddate>19871101</enddate><creator>Stanley, J.C</creator><creator>Markovic, J</creator><creator>Gutknecht, A.M</creator><creator>Lozeman, F.J</creator><scope>FBQ</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>7U7</scope><scope>C1K</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>19871101</creationdate><title>Stimulation of glycogenolysis in isolated hepatocytes by adenosine and one of its analogues is inhibited by caffeine</title><author>Stanley, J.C ; Markovic, J ; Gutknecht, A.M ; Lozeman, F.J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c449t-57b4eb5db4008d8b67707be1afbccc16ffe6c0bb5b135072c34a353b8d7359a33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>adenosine</topic><topic>Adenosine - analogs & derivatives</topic><topic>Adenosine - antagonists & inhibitors</topic><topic>Adenosine - pharmacology</topic><topic>Adenosine Deaminase - pharmacology</topic><topic>Adenosine-5'-(N-ethylcarboxamide)</topic><topic>Animals</topic><topic>caffeine</topic><topic>Caffeine - pharmacology</topic><topic>Cell Separation</topic><topic>Dose-Response Relationship, Drug</topic><topic>Enzyme Activation - drug effects</topic><topic>Glucagon - pharmacology</topic><topic>glycogenolysis</topic><topic>In Vitro Techniques</topic><topic>inhibition</topic><topic>liver</topic><topic>Liver - drug effects</topic><topic>Liver - metabolism</topic><topic>Liver Glycogen - metabolism</topic><topic>Male</topic><topic>Phenylisopropyladenosine - pharmacology</topic><topic>Phosphorylases - antagonists & inhibitors</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>stimulation</topic><topic>Stimulation, Chemical</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Stanley, J.C</creatorcontrib><creatorcontrib>Markovic, J</creatorcontrib><creatorcontrib>Gutknecht, A.M</creatorcontrib><creatorcontrib>Lozeman, F.J</creatorcontrib><collection>AGRIS</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Biochemical journal</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Stanley, J.C</au><au>Markovic, J</au><au>Gutknecht, A.M</au><au>Lozeman, F.J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Stimulation of glycogenolysis in isolated hepatocytes by adenosine and one of its analogues is inhibited by caffeine</atitle><jtitle>Biochemical journal</jtitle><addtitle>Biochem J</addtitle><date>1987-11-01</date><risdate>1987</risdate><volume>247</volume><issue>3</issue><spage>779</spage><epage>783</epage><pages>779-783</pages><issn>0264-6021</issn><eissn>1470-8728</eissn><abstract>The adenosine analogues 5'-(N-ethyl)carboxamidoadenosine (NECA) and N6-(phenylisopropyl)adenosine (PIA) activate glycogen phosphorylase 5-fold and 4.2-fold respectively in rat hepatocytes incubated in the absence of endogenous adenosine. Half-maximally effective concentrations are 0.5 microM for NECA and 20 microM for PIA, demonstrating the presence of A2-adenosine receptors. Exogenous adenosine activates phosphorylase 4.6-fold, but high rates of adenosine disappearance from the medium render estimates of its half-maximally effective concentration unreliable. These effects of NECA and adenosine are inhibited by 0.1 mM-caffeine. Activation of phosphorylase by a physiological concentration of adenosine (3.3 microM) was 50% inhibited by a physiological concentration of caffeine (35 microM).</abstract><cop>England</cop><pmid>3426562</pmid><doi>10.1042/bj2470779</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0264-6021 |
| ispartof | Biochemical journal, 1987-11, Vol.247 (3), p.779-783 |
| issn | 0264-6021 1470-8728 |
| language | eng |
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| source | MEDLINE; PMC (PubMed Central); EZB-FREE-00999 freely available EZB journals; Alma/SFX Local Collection |
| subjects | adenosine Adenosine - analogs & derivatives Adenosine - antagonists & inhibitors Adenosine - pharmacology Adenosine Deaminase - pharmacology Adenosine-5'-(N-ethylcarboxamide) Animals caffeine Caffeine - pharmacology Cell Separation Dose-Response Relationship, Drug Enzyme Activation - drug effects Glucagon - pharmacology glycogenolysis In Vitro Techniques inhibition liver Liver - drug effects Liver - metabolism Liver Glycogen - metabolism Male Phenylisopropyladenosine - pharmacology Phosphorylases - antagonists & inhibitors Rats Rats, Inbred Strains stimulation Stimulation, Chemical |
| title | Stimulation of glycogenolysis in isolated hepatocytes by adenosine and one of its analogues is inhibited by caffeine |
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