Picomolar-affinity binding and inhibition of adenylate cyclase activity by melatonin in Syrian hamster hypothalamus
1. The effect of melatonin on forskolin-stimulated adenylate cyclase activity was measured in homogenates of Syrian hamster hypothalamus. In addition, the saturation binding characteristics of the melatonin receptor ligand, [125I]iodomelatonin, was examined using an incubation temperature (30 degree...
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| Veröffentlicht in: | Cellular and molecular neurobiology 1990-12, Vol.10 (4), p.553-558 |
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| description | 1. The effect of melatonin on forskolin-stimulated adenylate cyclase activity was measured in homogenates of Syrian hamster hypothalamus. In addition, the saturation binding characteristics of the melatonin receptor ligand, [125I]iodomelatonin, was examined using an incubation temperature (30 degrees C) similar to that used in enzyme assays. 2. At concentrations ranging from 10 pM to 1 nM, melatonin caused a significant decrease in stimulated adenylate cyclase activity with a maximum inhibition of approximately 22%. 3. Binding experiments utilizing [125I]iodomelatonin in a range of approximately 5-80 pM indicated a single class of high-affinity sites: Kd = 55 +/- 9 pM, Bmax = 1.1 +/- 0.3 fmol/mg protein. 4. The ability of picomolar concentrations of melatonin to inhibit forskolin-stimulated adenylate cyclase activity suggests that this affect is mediated by picomolar-affinity receptor binding sites for this hormone in the hypothalamus. |
| doi_str_mv | 10.1007/BF00712848 |
| format | Article |
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P ; HASHEMI, F</creator><creatorcontrib>NILES, L. P ; HASHEMI, F</creatorcontrib><description>1. The effect of melatonin on forskolin-stimulated adenylate cyclase activity was measured in homogenates of Syrian hamster hypothalamus. In addition, the saturation binding characteristics of the melatonin receptor ligand, [125I]iodomelatonin, was examined using an incubation temperature (30 degrees C) similar to that used in enzyme assays. 2. At concentrations ranging from 10 pM to 1 nM, melatonin caused a significant decrease in stimulated adenylate cyclase activity with a maximum inhibition of approximately 22%. 3. Binding experiments utilizing [125I]iodomelatonin in a range of approximately 5-80 pM indicated a single class of high-affinity sites: Kd = 55 +/- 9 pM, Bmax = 1.1 +/- 0.3 fmol/mg protein. 4. The ability of picomolar concentrations of melatonin to inhibit forskolin-stimulated adenylate cyclase activity suggests that this affect is mediated by picomolar-affinity receptor binding sites for this hormone in the hypothalamus.</description><identifier>ISSN: 0272-4340</identifier><identifier>EISSN: 1573-6830</identifier><identifier>DOI: 10.1007/BF00712848</identifier><identifier>PMID: 1709064</identifier><identifier>CODEN: CMNEDI</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject>1-Methyl-3-isobutylxanthine - antagonists & inhibitors ; 550201 - Biochemistry- Tracer Techniques ; adenylate cyclase ; Adenylyl Cyclase Inhibitors ; AFFINITY ; AMINES ; ANIMALS ; AROMATICS ; AZAARENES ; AZOLES ; BASIC BIOLOGICAL SCIENCES ; BETA DECAY RADIOISOTOPES ; Binding Sites ; BIOCHEMICAL REACTION KINETICS ; Biological and medical sciences ; BODY ; BRAIN ; CENTRAL NERVOUS SYSTEM ; Colforsin - antagonists & inhibitors ; Colforsin - pharmacology ; Cricetinae ; CYCLASES ; DAYS LIVING RADIOISOTOPES ; ELECTRON CAPTURE RADIOISOTOPES ; ENZYME ACTIVITY ; ENZYMES ; Fundamental and applied biological sciences. Psychology ; HAMSTERS ; HETEROCYCLIC COMPOUNDS ; Hormones and neuropeptides. Regulation ; HYPOTHALAMUS ; Hypothalamus - drug effects ; Hypothalamus - metabolism ; Hypothalamus. Hypophysis. Epiphysis. Urophysis ; INDOLES ; INHIBITION ; INTERMEDIATE MASS NUCLEI ; INTERNAL CONVERSION RADIOISOTOPES ; IODINE 125 ; IODINE ISOTOPES ; Iodine Radioisotopes ; ISOTOPE APPLICATIONS ; ISOTOPES ; KINETICS ; LIGANDS ; LYASES ; Male ; MAMMALS ; MELATONIN ; Melatonin - pharmacology ; MEMBRANE PROTEINS ; Mesocricetus ; NERVOUS SYSTEM ; NUCLEI ; ODD-EVEN NUCLEI ; ORGANIC COMPOUNDS ; ORGANIC NITROGEN COMPOUNDS ; ORGANS ; PROTEINS ; PYRROLES ; RADIOASSAY ; RADIOISOTOPES ; Radioligand Assay ; REACTION KINETICS ; RECEPTORS ; Receptors, Melatonin ; Receptors, Neurotransmitter - drug effects ; RODENTS ; TRACER TECHNIQUES ; TRYPTAMINES ; VERTEBRATES ; Vertebrates: endocrinology</subject><ispartof>Cellular and molecular neurobiology, 1990-12, Vol.10 (4), p.553-558</ispartof><rights>1991 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c370t-d23c5abe5c9d1a9cd51d1b8dffb2bddbc69fb43cd3abb847d3471450fafa044e3</citedby><cites>FETCH-LOGICAL-c370t-d23c5abe5c9d1a9cd51d1b8dffb2bddbc69fb43cd3abb847d3471450fafa044e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,776,780,881,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19827591$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1709064$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://www.osti.gov/biblio/5639742$$D View this record in Osti.gov$$Hfree_for_read</backlink></links><search><creatorcontrib>NILES, L. P</creatorcontrib><creatorcontrib>HASHEMI, F</creatorcontrib><title>Picomolar-affinity binding and inhibition of adenylate cyclase activity by melatonin in Syrian hamster hypothalamus</title><title>Cellular and molecular neurobiology</title><addtitle>Cell Mol Neurobiol</addtitle><description>1. The effect of melatonin on forskolin-stimulated adenylate cyclase activity was measured in homogenates of Syrian hamster hypothalamus. In addition, the saturation binding characteristics of the melatonin receptor ligand, [125I]iodomelatonin, was examined using an incubation temperature (30 degrees C) similar to that used in enzyme assays. 2. At concentrations ranging from 10 pM to 1 nM, melatonin caused a significant decrease in stimulated adenylate cyclase activity with a maximum inhibition of approximately 22%. 3. Binding experiments utilizing [125I]iodomelatonin in a range of approximately 5-80 pM indicated a single class of high-affinity sites: Kd = 55 +/- 9 pM, Bmax = 1.1 +/- 0.3 fmol/mg protein. 4. The ability of picomolar concentrations of melatonin to inhibit forskolin-stimulated adenylate cyclase activity suggests that this affect is mediated by picomolar-affinity receptor binding sites for this hormone in the hypothalamus.</description><subject>1-Methyl-3-isobutylxanthine - antagonists & inhibitors</subject><subject>550201 - Biochemistry- Tracer Techniques</subject><subject>adenylate cyclase</subject><subject>Adenylyl Cyclase Inhibitors</subject><subject>AFFINITY</subject><subject>AMINES</subject><subject>ANIMALS</subject><subject>AROMATICS</subject><subject>AZAARENES</subject><subject>AZOLES</subject><subject>BASIC BIOLOGICAL SCIENCES</subject><subject>BETA DECAY RADIOISOTOPES</subject><subject>Binding Sites</subject><subject>BIOCHEMICAL REACTION KINETICS</subject><subject>Biological and medical sciences</subject><subject>BODY</subject><subject>BRAIN</subject><subject>CENTRAL NERVOUS SYSTEM</subject><subject>Colforsin - antagonists & inhibitors</subject><subject>Colforsin - pharmacology</subject><subject>Cricetinae</subject><subject>CYCLASES</subject><subject>DAYS LIVING RADIOISOTOPES</subject><subject>ELECTRON CAPTURE RADIOISOTOPES</subject><subject>ENZYME ACTIVITY</subject><subject>ENZYMES</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>HAMSTERS</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>Hormones and neuropeptides. Regulation</subject><subject>HYPOTHALAMUS</subject><subject>Hypothalamus - drug effects</subject><subject>Hypothalamus - metabolism</subject><subject>Hypothalamus. Hypophysis. Epiphysis. Urophysis</subject><subject>INDOLES</subject><subject>INHIBITION</subject><subject>INTERMEDIATE MASS NUCLEI</subject><subject>INTERNAL CONVERSION RADIOISOTOPES</subject><subject>IODINE 125</subject><subject>IODINE ISOTOPES</subject><subject>Iodine Radioisotopes</subject><subject>ISOTOPE APPLICATIONS</subject><subject>ISOTOPES</subject><subject>KINETICS</subject><subject>LIGANDS</subject><subject>LYASES</subject><subject>Male</subject><subject>MAMMALS</subject><subject>MELATONIN</subject><subject>Melatonin - pharmacology</subject><subject>MEMBRANE PROTEINS</subject><subject>Mesocricetus</subject><subject>NERVOUS SYSTEM</subject><subject>NUCLEI</subject><subject>ODD-EVEN NUCLEI</subject><subject>ORGANIC COMPOUNDS</subject><subject>ORGANIC NITROGEN COMPOUNDS</subject><subject>ORGANS</subject><subject>PROTEINS</subject><subject>PYRROLES</subject><subject>RADIOASSAY</subject><subject>RADIOISOTOPES</subject><subject>Radioligand Assay</subject><subject>REACTION KINETICS</subject><subject>RECEPTORS</subject><subject>Receptors, Melatonin</subject><subject>Receptors, Neurotransmitter - drug effects</subject><subject>RODENTS</subject><subject>TRACER TECHNIQUES</subject><subject>TRYPTAMINES</subject><subject>VERTEBRATES</subject><subject>Vertebrates: endocrinology</subject><issn>0272-4340</issn><issn>1573-6830</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0cGL1DAUBvAgyjquXrwLQdCD0DVpkqY56uKqsLAL6rm8vCQ20iZjk1nof291BuboJS_w_d67fIS85OyKM6bff7zZXt72sn9Edlxp0XS9YI_JjrW6baSQ7Cl5VsovxphhTF2QC663Xyd3pNxHzHOeYGkghJhiXamNycX0k0JyNKYx2lhjTjQHCs6ndYLqKa44QfEUsMaHf0srnf0W5RTTtkW_rUuEREeYS_ULHdd9riNMMB_Kc_IkwFT8i9O8JD9uPn2__tLc3n3-ev3htkGhWW1cK1CB9QqN42DQKe647V0ItrXOWexMsFKgE2BtL7UTUnOpWIAATEovLsnr491cahwKxupxxJySxzqoThgt2w29PaL9kn8ffKnDHAv6aYLk86EMPROCGcP-C7nqtTad2OC7I8Qll7L4MOyXOMOyDpwNf_sazn1t-NXp6sHO3p3psaAtf3PKoSBMYYGEsZyZ6VutDBd_APVGn3A</recordid><startdate>19901201</startdate><enddate>19901201</enddate><creator>NILES, L. P</creator><creator>HASHEMI, F</creator><general>Springer</general><scope>IQODW</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>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>M7Z</scope><scope>P64</scope><scope>7X8</scope><scope>OTOTI</scope></search><sort><creationdate>19901201</creationdate><title>Picomolar-affinity binding and inhibition of adenylate cyclase activity by melatonin in Syrian hamster hypothalamus</title><author>NILES, L. P ; HASHEMI, F</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c370t-d23c5abe5c9d1a9cd51d1b8dffb2bddbc69fb43cd3abb847d3471450fafa044e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>1-Methyl-3-isobutylxanthine - antagonists & inhibitors</topic><topic>550201 - Biochemistry- Tracer Techniques</topic><topic>adenylate cyclase</topic><topic>Adenylyl Cyclase Inhibitors</topic><topic>AFFINITY</topic><topic>AMINES</topic><topic>ANIMALS</topic><topic>AROMATICS</topic><topic>AZAARENES</topic><topic>AZOLES</topic><topic>BASIC BIOLOGICAL SCIENCES</topic><topic>BETA DECAY RADIOISOTOPES</topic><topic>Binding Sites</topic><topic>BIOCHEMICAL REACTION KINETICS</topic><topic>Biological and medical sciences</topic><topic>BODY</topic><topic>BRAIN</topic><topic>CENTRAL NERVOUS SYSTEM</topic><topic>Colforsin - antagonists & inhibitors</topic><topic>Colforsin - pharmacology</topic><topic>Cricetinae</topic><topic>CYCLASES</topic><topic>DAYS LIVING RADIOISOTOPES</topic><topic>ELECTRON CAPTURE RADIOISOTOPES</topic><topic>ENZYME ACTIVITY</topic><topic>ENZYMES</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>HAMSTERS</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>Hormones and neuropeptides. Regulation</topic><topic>HYPOTHALAMUS</topic><topic>Hypothalamus - drug effects</topic><topic>Hypothalamus - metabolism</topic><topic>Hypothalamus. Hypophysis. Epiphysis. Urophysis</topic><topic>INDOLES</topic><topic>INHIBITION</topic><topic>INTERMEDIATE MASS NUCLEI</topic><topic>INTERNAL CONVERSION RADIOISOTOPES</topic><topic>IODINE 125</topic><topic>IODINE ISOTOPES</topic><topic>Iodine Radioisotopes</topic><topic>ISOTOPE APPLICATIONS</topic><topic>ISOTOPES</topic><topic>KINETICS</topic><topic>LIGANDS</topic><topic>LYASES</topic><topic>Male</topic><topic>MAMMALS</topic><topic>MELATONIN</topic><topic>Melatonin - pharmacology</topic><topic>MEMBRANE PROTEINS</topic><topic>Mesocricetus</topic><topic>NERVOUS SYSTEM</topic><topic>NUCLEI</topic><topic>ODD-EVEN NUCLEI</topic><topic>ORGANIC COMPOUNDS</topic><topic>ORGANIC NITROGEN COMPOUNDS</topic><topic>ORGANS</topic><topic>PROTEINS</topic><topic>PYRROLES</topic><topic>RADIOASSAY</topic><topic>RADIOISOTOPES</topic><topic>Radioligand Assay</topic><topic>REACTION KINETICS</topic><topic>RECEPTORS</topic><topic>Receptors, Melatonin</topic><topic>Receptors, Neurotransmitter - drug effects</topic><topic>RODENTS</topic><topic>TRACER TECHNIQUES</topic><topic>TRYPTAMINES</topic><topic>VERTEBRATES</topic><topic>Vertebrates: endocrinology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>NILES, L. P</creatorcontrib><creatorcontrib>HASHEMI, F</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>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biochemistry Abstracts 1</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><collection>OSTI.GOV</collection><jtitle>Cellular and molecular neurobiology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>NILES, L. P</au><au>HASHEMI, F</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Picomolar-affinity binding and inhibition of adenylate cyclase activity by melatonin in Syrian hamster hypothalamus</atitle><jtitle>Cellular and molecular neurobiology</jtitle><addtitle>Cell Mol Neurobiol</addtitle><date>1990-12-01</date><risdate>1990</risdate><volume>10</volume><issue>4</issue><spage>553</spage><epage>558</epage><pages>553-558</pages><issn>0272-4340</issn><eissn>1573-6830</eissn><coden>CMNEDI</coden><abstract>1. The effect of melatonin on forskolin-stimulated adenylate cyclase activity was measured in homogenates of Syrian hamster hypothalamus. In addition, the saturation binding characteristics of the melatonin receptor ligand, [125I]iodomelatonin, was examined using an incubation temperature (30 degrees C) similar to that used in enzyme assays. 2. At concentrations ranging from 10 pM to 1 nM, melatonin caused a significant decrease in stimulated adenylate cyclase activity with a maximum inhibition of approximately 22%. 3. Binding experiments utilizing [125I]iodomelatonin in a range of approximately 5-80 pM indicated a single class of high-affinity sites: Kd = 55 +/- 9 pM, Bmax = 1.1 +/- 0.3 fmol/mg protein. 4. The ability of picomolar concentrations of melatonin to inhibit forskolin-stimulated adenylate cyclase activity suggests that this affect is mediated by picomolar-affinity receptor binding sites for this hormone in the hypothalamus.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>1709064</pmid><doi>10.1007/BF00712848</doi><tpages>6</tpages></addata></record> |
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| ispartof | Cellular and molecular neurobiology, 1990-12, Vol.10 (4), p.553-558 |
| issn | 0272-4340 1573-6830 |
| language | eng |
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| subjects | 1-Methyl-3-isobutylxanthine - antagonists & inhibitors 550201 - Biochemistry- Tracer Techniques adenylate cyclase Adenylyl Cyclase Inhibitors AFFINITY AMINES ANIMALS AROMATICS AZAARENES AZOLES BASIC BIOLOGICAL SCIENCES BETA DECAY RADIOISOTOPES Binding Sites BIOCHEMICAL REACTION KINETICS Biological and medical sciences BODY BRAIN CENTRAL NERVOUS SYSTEM Colforsin - antagonists & inhibitors Colforsin - pharmacology Cricetinae CYCLASES DAYS LIVING RADIOISOTOPES ELECTRON CAPTURE RADIOISOTOPES ENZYME ACTIVITY ENZYMES Fundamental and applied biological sciences. Psychology HAMSTERS HETEROCYCLIC COMPOUNDS Hormones and neuropeptides. Regulation HYPOTHALAMUS Hypothalamus - drug effects Hypothalamus - metabolism Hypothalamus. Hypophysis. Epiphysis. Urophysis INDOLES INHIBITION INTERMEDIATE MASS NUCLEI INTERNAL CONVERSION RADIOISOTOPES IODINE 125 IODINE ISOTOPES Iodine Radioisotopes ISOTOPE APPLICATIONS ISOTOPES KINETICS LIGANDS LYASES Male MAMMALS MELATONIN Melatonin - pharmacology MEMBRANE PROTEINS Mesocricetus NERVOUS SYSTEM NUCLEI ODD-EVEN NUCLEI ORGANIC COMPOUNDS ORGANIC NITROGEN COMPOUNDS ORGANS PROTEINS PYRROLES RADIOASSAY RADIOISOTOPES Radioligand Assay REACTION KINETICS RECEPTORS Receptors, Melatonin Receptors, Neurotransmitter - drug effects RODENTS TRACER TECHNIQUES TRYPTAMINES VERTEBRATES Vertebrates: endocrinology |
| title | Picomolar-affinity binding and inhibition of adenylate cyclase activity by melatonin in Syrian hamster hypothalamus |
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