(125)I-spectramide: A novel benzamide displaying potent and selective effects at the D sub 2 dopamine receptor
The new substituted benzamide Spectramide, (N-(2-(4-iodobenzyl-N-methylamino)-2-methoxy-4-ethyl)-5-chloro-methylamine benzamide) labelled with {sup 125}I was used as a potent and highly selective dopamine-D{sub 2} receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic...
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| Veröffentlicht in: | Life sciences (1973) 1989-01, Vol.45:19 |
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| container_title | Life sciences (1973) |
| container_volume | 45:19 |
| creator | Sanchez-Roa, P.M. Grigoriadis, D.E. Wilson, A.A. Sharkey, J. Dannals, R.F. Villemagne, Victor, L. Wong, D.F. Wagner, H.N. Jr Kuhar, M.J. |
| description | The new substituted benzamide Spectramide, (N-(2-(4-iodobenzyl-N-methylamino)-2-methoxy-4-ethyl)-5-chloro-methylamine benzamide) labelled with {sup 125}I was used as a potent and highly selective dopamine-D{sub 2} receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D{sub 1} or dopamine-uptake site. Drugs known to interact with other receptor system were weak competitors of the binding, while binding was potently inhibited by other D{sub 2} antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D{sub 2} receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT. |
| doi_str_mv | 10.1016/0024-3205(89)90523-7 |
| format | Article |
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Jr ; Kuhar, M.J.</creator><creatorcontrib>Sanchez-Roa, P.M. ; Grigoriadis, D.E. ; Wilson, A.A. ; Sharkey, J. ; Dannals, R.F. ; Villemagne, Victor, L. ; Wong, D.F. ; Wagner, H.N. Jr ; Kuhar, M.J.</creatorcontrib><description>The new substituted benzamide Spectramide, (N-(2-(4-iodobenzyl-N-methylamino)-2-methoxy-4-ethyl)-5-chloro-methylamine benzamide) labelled with {sup 125}I was used as a potent and highly selective dopamine-D{sub 2} receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D{sub 1} or dopamine-uptake site. Drugs known to interact with other receptor system were weak competitors of the binding, while binding was potently inhibited by other D{sub 2} antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D{sub 2} receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/0024-3205(89)90523-7</identifier><language>eng</language><publisher>United States</publisher><subject>550201 - Biochemistry- Tracer Techniques ; 550601 - Medicine- Unsealed Radionuclides in Diagnostics ; AMINES ; ANIMALS ; AROMATICS ; AUTONOMIC NERVOUS SYSTEM AGENTS ; BASIC BIOLOGICAL SCIENCES ; BETA DECAY RADIOISOTOPES ; BIOCHEMICAL REACTION KINETICS ; CARDIOTONICS ; CARDIOVASCULAR AGENTS ; COMPUTERIZED TOMOGRAPHY ; DAYS LIVING RADIOISOTOPES ; DIAGNOSTIC TECHNIQUES ; DOPAMINE ; DRUGS ; ELECTRON CAPTURE RADIOISOTOPES ; EMISSION COMPUTED TOMOGRAPHY ; HYDROXY COMPOUNDS ; INTERMEDIATE MASS NUCLEI ; IODINE 125 ; IODINE ISOTOPES ; ISOTOPE APPLICATIONS ; ISOTOPES ; KINETICS ; LABELLED COMPOUNDS ; MAMMALS ; MEMBRANE PROTEINS ; NEUROREGULATORS ; NUCLEI ; ODD-EVEN NUCLEI ; ORGANIC COMPOUNDS ; PHENOLS ; POLYPHENOLS ; POSITRON COMPUTED TOMOGRAPHY ; PROTEINS ; RADIOISOTOPES ; RADIOLOGY AND NUCLEAR MEDICINE ; RADIOPHARMACEUTICALS ; RATS ; REACTION KINETICS ; RECEPTORS ; RODENTS ; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY ; SYMPATHOMIMETICS ; TOMOGRAPHY ; TRACER TECHNIQUES ; VERTEBRATES</subject><ispartof>Life sciences (1973), 1989-01, Vol.45:19</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,778,782,883,27907,27908</link.rule.ids><backlink>$$Uhttps://www.osti.gov/biblio/7027013$$D View this record in Osti.gov$$Hfree_for_read</backlink></links><search><creatorcontrib>Sanchez-Roa, P.M.</creatorcontrib><creatorcontrib>Grigoriadis, D.E.</creatorcontrib><creatorcontrib>Wilson, A.A.</creatorcontrib><creatorcontrib>Sharkey, J.</creatorcontrib><creatorcontrib>Dannals, R.F.</creatorcontrib><creatorcontrib>Villemagne, Victor, L.</creatorcontrib><creatorcontrib>Wong, D.F.</creatorcontrib><creatorcontrib>Wagner, H.N. Jr</creatorcontrib><creatorcontrib>Kuhar, M.J.</creatorcontrib><title>(125)I-spectramide: A novel benzamide displaying potent and selective effects at the D sub 2 dopamine receptor</title><title>Life sciences (1973)</title><description>The new substituted benzamide Spectramide, (N-(2-(4-iodobenzyl-N-methylamino)-2-methoxy-4-ethyl)-5-chloro-methylamine benzamide) labelled with {sup 125}I was used as a potent and highly selective dopamine-D{sub 2} receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D{sub 1} or dopamine-uptake site. Drugs known to interact with other receptor system were weak competitors of the binding, while binding was potently inhibited by other D{sub 2} antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D{sub 2} receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.</description><subject>550201 - Biochemistry- Tracer Techniques</subject><subject>550601 - Medicine- Unsealed Radionuclides in Diagnostics</subject><subject>AMINES</subject><subject>ANIMALS</subject><subject>AROMATICS</subject><subject>AUTONOMIC NERVOUS SYSTEM AGENTS</subject><subject>BASIC BIOLOGICAL SCIENCES</subject><subject>BETA DECAY RADIOISOTOPES</subject><subject>BIOCHEMICAL REACTION KINETICS</subject><subject>CARDIOTONICS</subject><subject>CARDIOVASCULAR AGENTS</subject><subject>COMPUTERIZED TOMOGRAPHY</subject><subject>DAYS LIVING RADIOISOTOPES</subject><subject>DIAGNOSTIC TECHNIQUES</subject><subject>DOPAMINE</subject><subject>DRUGS</subject><subject>ELECTRON CAPTURE RADIOISOTOPES</subject><subject>EMISSION COMPUTED TOMOGRAPHY</subject><subject>HYDROXY COMPOUNDS</subject><subject>INTERMEDIATE MASS NUCLEI</subject><subject>IODINE 125</subject><subject>IODINE ISOTOPES</subject><subject>ISOTOPE APPLICATIONS</subject><subject>ISOTOPES</subject><subject>KINETICS</subject><subject>LABELLED COMPOUNDS</subject><subject>MAMMALS</subject><subject>MEMBRANE PROTEINS</subject><subject>NEUROREGULATORS</subject><subject>NUCLEI</subject><subject>ODD-EVEN NUCLEI</subject><subject>ORGANIC COMPOUNDS</subject><subject>PHENOLS</subject><subject>POLYPHENOLS</subject><subject>POSITRON COMPUTED TOMOGRAPHY</subject><subject>PROTEINS</subject><subject>RADIOISOTOPES</subject><subject>RADIOLOGY AND NUCLEAR MEDICINE</subject><subject>RADIOPHARMACEUTICALS</subject><subject>RATS</subject><subject>REACTION KINETICS</subject><subject>RECEPTORS</subject><subject>RODENTS</subject><subject>SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY</subject><subject>SYMPATHOMIMETICS</subject><subject>TOMOGRAPHY</subject><subject>TRACER TECHNIQUES</subject><subject>VERTEBRATES</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><recordid>eNqNjMFKAzEURYMoOFb_wMXDVbtIfUlM03EnVtG9-5Jm3tjImIR5saBf7yDi2tW9XM65QlwqXCpUq2tEfSONRjtft4sWrTbSHYlGrV0rcWXUsWj-kFNxxvyGiNY604g0V9ouniUXCnX077GjW7iDlA80wI7S188EXeQy-M-YXqHkSqmCTx0wDZMVDwTU91Nj8BXqnmAD_LEDDV0uk58IRgpUah7PxUnvB6aL35yJq8eHl_snmbnGLYdYKexDTml62zrUDpUx_4K-AURTTzg</recordid><startdate>19890101</startdate><enddate>19890101</enddate><creator>Sanchez-Roa, P.M.</creator><creator>Grigoriadis, D.E.</creator><creator>Wilson, A.A.</creator><creator>Sharkey, J.</creator><creator>Dannals, R.F.</creator><creator>Villemagne, Victor, L.</creator><creator>Wong, D.F.</creator><creator>Wagner, H.N. Jr</creator><creator>Kuhar, M.J.</creator><scope>OTOTI</scope></search><sort><creationdate>19890101</creationdate><title>(125)I-spectramide: A novel benzamide displaying potent and selective effects at the D sub 2 dopamine receptor</title><author>Sanchez-Roa, P.M. ; Grigoriadis, D.E. ; Wilson, A.A. ; Sharkey, J. ; Dannals, R.F. ; Villemagne, Victor, L. ; Wong, D.F. ; Wagner, H.N. Jr ; Kuhar, M.J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-osti_scitechconnect_70270133</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>550201 - Biochemistry- Tracer Techniques</topic><topic>550601 - Medicine- Unsealed Radionuclides in Diagnostics</topic><topic>AMINES</topic><topic>ANIMALS</topic><topic>AROMATICS</topic><topic>AUTONOMIC NERVOUS SYSTEM AGENTS</topic><topic>BASIC BIOLOGICAL SCIENCES</topic><topic>BETA DECAY RADIOISOTOPES</topic><topic>BIOCHEMICAL REACTION KINETICS</topic><topic>CARDIOTONICS</topic><topic>CARDIOVASCULAR AGENTS</topic><topic>COMPUTERIZED TOMOGRAPHY</topic><topic>DAYS LIVING RADIOISOTOPES</topic><topic>DIAGNOSTIC TECHNIQUES</topic><topic>DOPAMINE</topic><topic>DRUGS</topic><topic>ELECTRON CAPTURE RADIOISOTOPES</topic><topic>EMISSION COMPUTED TOMOGRAPHY</topic><topic>HYDROXY COMPOUNDS</topic><topic>INTERMEDIATE MASS NUCLEI</topic><topic>IODINE 125</topic><topic>IODINE ISOTOPES</topic><topic>ISOTOPE APPLICATIONS</topic><topic>ISOTOPES</topic><topic>KINETICS</topic><topic>LABELLED COMPOUNDS</topic><topic>MAMMALS</topic><topic>MEMBRANE PROTEINS</topic><topic>NEUROREGULATORS</topic><topic>NUCLEI</topic><topic>ODD-EVEN NUCLEI</topic><topic>ORGANIC COMPOUNDS</topic><topic>PHENOLS</topic><topic>POLYPHENOLS</topic><topic>POSITRON COMPUTED TOMOGRAPHY</topic><topic>PROTEINS</topic><topic>RADIOISOTOPES</topic><topic>RADIOLOGY AND NUCLEAR MEDICINE</topic><topic>RADIOPHARMACEUTICALS</topic><topic>RATS</topic><topic>REACTION KINETICS</topic><topic>RECEPTORS</topic><topic>RODENTS</topic><topic>SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY</topic><topic>SYMPATHOMIMETICS</topic><topic>TOMOGRAPHY</topic><topic>TRACER TECHNIQUES</topic><topic>VERTEBRATES</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sanchez-Roa, P.M.</creatorcontrib><creatorcontrib>Grigoriadis, D.E.</creatorcontrib><creatorcontrib>Wilson, A.A.</creatorcontrib><creatorcontrib>Sharkey, J.</creatorcontrib><creatorcontrib>Dannals, R.F.</creatorcontrib><creatorcontrib>Villemagne, Victor, L.</creatorcontrib><creatorcontrib>Wong, D.F.</creatorcontrib><creatorcontrib>Wagner, H.N. Jr</creatorcontrib><creatorcontrib>Kuhar, M.J.</creatorcontrib><collection>OSTI.GOV</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sanchez-Roa, P.M.</au><au>Grigoriadis, D.E.</au><au>Wilson, A.A.</au><au>Sharkey, J.</au><au>Dannals, R.F.</au><au>Villemagne, Victor, L.</au><au>Wong, D.F.</au><au>Wagner, H.N. Jr</au><au>Kuhar, M.J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>(125)I-spectramide: A novel benzamide displaying potent and selective effects at the D sub 2 dopamine receptor</atitle><jtitle>Life sciences (1973)</jtitle><date>1989-01-01</date><risdate>1989</risdate><volume>45:19</volume><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>The new substituted benzamide Spectramide, (N-(2-(4-iodobenzyl-N-methylamino)-2-methoxy-4-ethyl)-5-chloro-methylamine benzamide) labelled with {sup 125}I was used as a potent and highly selective dopamine-D{sub 2} receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D{sub 1} or dopamine-uptake site. Drugs known to interact with other receptor system were weak competitors of the binding, while binding was potently inhibited by other D{sub 2} antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D{sub 2} receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.</abstract><cop>United States</cop><doi>10.1016/0024-3205(89)90523-7</doi></addata></record> |
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| ispartof | Life sciences (1973), 1989-01, Vol.45:19 |
| issn | 0024-3205 1879-0631 |
| language | eng |
| recordid | cdi_osti_scitechconnect_7027013 |
| source | Elsevier ScienceDirect Journals |
| subjects | 550201 - Biochemistry- Tracer Techniques 550601 - Medicine- Unsealed Radionuclides in Diagnostics AMINES ANIMALS AROMATICS AUTONOMIC NERVOUS SYSTEM AGENTS BASIC BIOLOGICAL SCIENCES BETA DECAY RADIOISOTOPES BIOCHEMICAL REACTION KINETICS CARDIOTONICS CARDIOVASCULAR AGENTS COMPUTERIZED TOMOGRAPHY DAYS LIVING RADIOISOTOPES DIAGNOSTIC TECHNIQUES DOPAMINE DRUGS ELECTRON CAPTURE RADIOISOTOPES EMISSION COMPUTED TOMOGRAPHY HYDROXY COMPOUNDS INTERMEDIATE MASS NUCLEI IODINE 125 IODINE ISOTOPES ISOTOPE APPLICATIONS ISOTOPES KINETICS LABELLED COMPOUNDS MAMMALS MEMBRANE PROTEINS NEUROREGULATORS NUCLEI ODD-EVEN NUCLEI ORGANIC COMPOUNDS PHENOLS POLYPHENOLS POSITRON COMPUTED TOMOGRAPHY PROTEINS RADIOISOTOPES RADIOLOGY AND NUCLEAR MEDICINE RADIOPHARMACEUTICALS RATS REACTION KINETICS RECEPTORS RODENTS SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY SYMPATHOMIMETICS TOMOGRAPHY TRACER TECHNIQUES VERTEBRATES |
| title | (125)I-spectramide: A novel benzamide displaying potent and selective effects at the D sub 2 dopamine receptor |
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