Adrenergic and Dopaminergic Properties of Dopamine Sulfoconjugates

The 3- and 4-sulfate esters of dopamine (DA-3-SO4 and DA-4-SO4, respectively), the two main metabolites of DA, were evaluated for potential intrinsic or indirect catecholaminergic activities. Both compounds lacked any appreciable affinities for α1, α2, β1, β2 and DA-2 receptors. In the superfused [H...

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Veröffentlicht in:Journal of cardiovascular pharmacology 1985-11, Vol.7 (6), p.1198-1204
Hauptverfasser: Kyncl, John J, Buckner, Steven A, Brondyk, Harold, Kerkman, Daniel J, DeBernardis, John F, Bush, Eugene N, Kuchel, Otto
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container_end_page 1204
container_issue 6
container_start_page 1198
container_title Journal of cardiovascular pharmacology
container_volume 7
creator Kyncl, John J
Buckner, Steven A
Brondyk, Harold
Kerkman, Daniel J
DeBernardis, John F
Bush, Eugene N
Kuchel, Otto
description The 3- and 4-sulfate esters of dopamine (DA-3-SO4 and DA-4-SO4, respectively), the two main metabolites of DA, were evaluated for potential intrinsic or indirect catecholaminergic activities. Both compounds lacked any appreciable affinities for α1, α2, β1, β2 and DA-2 receptors. In the superfused [H]norepinephrine-preloaded dog saphenous vein, both dopamine sulfates were devoid of any intrinsic inhibitory activity such as observed with dopamine pre- and postsynaptically. In addition, they did not displace the labeled vesicular neurotransmitter as did dopamine. In anesthetized dogs the two compounds failed to stimulate either the dopaminergic receptors (DA-1) of mesenteric vascular beds or the adrenergic receptors mediating the vasodilatory and pressor responses to dopamine. ConclusionIn our experimental conditions DA-3-SO4 and DA-4-SO4, the products of dopamine sulfoconjugation, lacked any demonstrable intrinsic affinity and/or efficacy on the dopaminergic and adrenergic receptors directly or indirectly (a) through their metabolic transformation or (b) through displacement of endogenous neurotransmitter.
doi_str_mv 10.1097/00005344-198511000-00030
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Both compounds lacked any appreciable affinities for α1, α2, β1, β2 and DA-2 receptors. In the superfused [H]norepinephrine-preloaded dog saphenous vein, both dopamine sulfates were devoid of any intrinsic inhibitory activity such as observed with dopamine pre- and postsynaptically. In addition, they did not displace the labeled vesicular neurotransmitter as did dopamine. In anesthetized dogs the two compounds failed to stimulate either the dopaminergic receptors (DA-1) of mesenteric vascular beds or the adrenergic receptors mediating the vasodilatory and pressor responses to dopamine. ConclusionIn our experimental conditions DA-3-SO4 and DA-4-SO4, the products of dopamine sulfoconjugation, lacked any demonstrable intrinsic affinity and/or efficacy on the dopaminergic and adrenergic receptors directly or indirectly (a) through their metabolic transformation or (b) through displacement of endogenous neurotransmitter.</description><identifier>ISSN: 0160-2446</identifier><identifier>EISSN: 1533-4023</identifier><identifier>DOI: 10.1097/00005344-198511000-00030</identifier><identifier>PMID: 2418311</identifier><identifier>CODEN: JCPCDT</identifier><language>eng</language><publisher>Philadelphia, PA: Lippincott-Raven Publishers</publisher><subject>Animals ; Biological and medical sciences ; Catecholaminergic system ; Dogs ; Dopamine - analogs &amp; derivatives ; Dopamine - metabolism ; Dopamine - pharmacology ; In Vitro Techniques ; Male ; Medical sciences ; Muscle, Smooth, Vascular - drug effects ; Muscle, Smooth, Vascular - metabolism ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Rats ; Rats, Inbred Strains ; Receptors, Adrenergic, alpha - metabolism ; Receptors, Adrenergic, beta - metabolism ; Receptors, Dopamine - drug effects ; Receptors, Dopamine - metabolism ; Splanchnic Circulation - drug effects ; Sympathetic Nervous System - drug effects</subject><ispartof>Journal of cardiovascular pharmacology, 1985-11, Vol.7 (6), p.1198-1204</ispartof><rights>Lippincott-Raven Publishers.</rights><rights>1986 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4340-60d5bef4432704fead3546e00faaa96ed38e276ef9d210f98b5a4c4038359dbb3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttp://ovidsp.ovid.com/ovidweb.cgi?T=JS&amp;NEWS=n&amp;CSC=Y&amp;PAGE=fulltext&amp;D=ovft&amp;AN=00005344-198511000-00030$$EHTML$$P50$$Gwolterskluwer$$H</linktohtml><link.rule.ids>314,776,780,4594,27903,27904,65209</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&amp;idt=8711592$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2418311$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kyncl, John J</creatorcontrib><creatorcontrib>Buckner, Steven A</creatorcontrib><creatorcontrib>Brondyk, Harold</creatorcontrib><creatorcontrib>Kerkman, Daniel J</creatorcontrib><creatorcontrib>DeBernardis, John F</creatorcontrib><creatorcontrib>Bush, Eugene N</creatorcontrib><creatorcontrib>Kuchel, Otto</creatorcontrib><title>Adrenergic and Dopaminergic Properties of Dopamine Sulfoconjugates</title><title>Journal of cardiovascular pharmacology</title><addtitle>J Cardiovasc Pharmacol</addtitle><description>The 3- and 4-sulfate esters of dopamine (DA-3-SO4 and DA-4-SO4, respectively), the two main metabolites of DA, were evaluated for potential intrinsic or indirect catecholaminergic activities. Both compounds lacked any appreciable affinities for α1, α2, β1, β2 and DA-2 receptors. In the superfused [H]norepinephrine-preloaded dog saphenous vein, both dopamine sulfates were devoid of any intrinsic inhibitory activity such as observed with dopamine pre- and postsynaptically. In addition, they did not displace the labeled vesicular neurotransmitter as did dopamine. In anesthetized dogs the two compounds failed to stimulate either the dopaminergic receptors (DA-1) of mesenteric vascular beds or the adrenergic receptors mediating the vasodilatory and pressor responses to dopamine. ConclusionIn our experimental conditions DA-3-SO4 and DA-4-SO4, the products of dopamine sulfoconjugation, lacked any demonstrable intrinsic affinity and/or efficacy on the dopaminergic and adrenergic receptors directly or indirectly (a) through their metabolic transformation or (b) through displacement of endogenous neurotransmitter.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Catecholaminergic system</subject><subject>Dogs</subject><subject>Dopamine - analogs &amp; derivatives</subject><subject>Dopamine - metabolism</subject><subject>Dopamine - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Muscle, Smooth, Vascular - metabolism</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Adrenergic, alpha - metabolism</subject><subject>Receptors, Adrenergic, beta - metabolism</subject><subject>Receptors, Dopamine - drug effects</subject><subject>Receptors, Dopamine - metabolism</subject><subject>Splanchnic Circulation - drug effects</subject><subject>Sympathetic Nervous System - drug effects</subject><issn>0160-2446</issn><issn>1533-4023</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1985</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kV1LwzAUhoMoc05_gtAL8a560ny0vZzzEwYK6nVI25Ots21q0jL891ZXd2cghJz3OTnwhJCAwhWFNL6GYQnGeUjTRFA63MJhMzggUyoYCzlE7JBMgUoII87lMTnxfgNAuYjlhEwiThNG6ZTczAuHDbpVmQe6KYJb2-q6HAsvzrbouhJ9YM0-Cl77ytjcNpt-pTv0p-TI6Mrj2XjOyPv93dviMVw-Pzwt5ssw54xDKKEQGRrOWRQDN6gLJrhEAKO1TiUWLMEolmjSIqJg0iQTmuccWMJEWmQZm5HL3buts589-k7Vpc-xqnSDtvcqlkKmkrEBTHZg7qz3Do1qXVlr96UoqB996k-f2utTv_qG1vNxRp_VWOwbR19DfjHm2ue6Mk43een3WBJTKtJowPgO29qqQ-c_qn6LTq1RV91a_fd57Bv8Load</recordid><startdate>198511</startdate><enddate>198511</enddate><creator>Kyncl, John J</creator><creator>Buckner, Steven A</creator><creator>Brondyk, Harold</creator><creator>Kerkman, Daniel J</creator><creator>DeBernardis, John F</creator><creator>Bush, Eugene N</creator><creator>Kuchel, Otto</creator><general>Lippincott-Raven Publishers</general><general>Lippincott</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>7X8</scope></search><sort><creationdate>198511</creationdate><title>Adrenergic and Dopaminergic Properties of Dopamine Sulfoconjugates</title><author>Kyncl, John J ; Buckner, Steven A ; Brondyk, Harold ; Kerkman, Daniel J ; DeBernardis, John F ; Bush, Eugene N ; Kuchel, Otto</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4340-60d5bef4432704fead3546e00faaa96ed38e276ef9d210f98b5a4c4038359dbb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Catecholaminergic system</topic><topic>Dogs</topic><topic>Dopamine - analogs &amp; derivatives</topic><topic>Dopamine - metabolism</topic><topic>Dopamine - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Muscle, Smooth, Vascular - metabolism</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Adrenergic, alpha - metabolism</topic><topic>Receptors, Adrenergic, beta - metabolism</topic><topic>Receptors, Dopamine - drug effects</topic><topic>Receptors, Dopamine - metabolism</topic><topic>Splanchnic Circulation - drug effects</topic><topic>Sympathetic Nervous System - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kyncl, John J</creatorcontrib><creatorcontrib>Buckner, Steven A</creatorcontrib><creatorcontrib>Brondyk, Harold</creatorcontrib><creatorcontrib>Kerkman, Daniel J</creatorcontrib><creatorcontrib>DeBernardis, John F</creatorcontrib><creatorcontrib>Bush, Eugene N</creatorcontrib><creatorcontrib>Kuchel, Otto</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>MEDLINE - Academic</collection><jtitle>Journal of cardiovascular pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kyncl, John J</au><au>Buckner, Steven A</au><au>Brondyk, Harold</au><au>Kerkman, Daniel J</au><au>DeBernardis, John F</au><au>Bush, Eugene N</au><au>Kuchel, Otto</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Adrenergic and Dopaminergic Properties of Dopamine Sulfoconjugates</atitle><jtitle>Journal of cardiovascular pharmacology</jtitle><addtitle>J Cardiovasc Pharmacol</addtitle><date>1985-11</date><risdate>1985</risdate><volume>7</volume><issue>6</issue><spage>1198</spage><epage>1204</epage><pages>1198-1204</pages><issn>0160-2446</issn><eissn>1533-4023</eissn><coden>JCPCDT</coden><abstract>The 3- and 4-sulfate esters of dopamine (DA-3-SO4 and DA-4-SO4, respectively), the two main metabolites of DA, were evaluated for potential intrinsic or indirect catecholaminergic activities. Both compounds lacked any appreciable affinities for α1, α2, β1, β2 and DA-2 receptors. In the superfused [H]norepinephrine-preloaded dog saphenous vein, both dopamine sulfates were devoid of any intrinsic inhibitory activity such as observed with dopamine pre- and postsynaptically. In addition, they did not displace the labeled vesicular neurotransmitter as did dopamine. In anesthetized dogs the two compounds failed to stimulate either the dopaminergic receptors (DA-1) of mesenteric vascular beds or the adrenergic receptors mediating the vasodilatory and pressor responses to dopamine. ConclusionIn our experimental conditions DA-3-SO4 and DA-4-SO4, the products of dopamine sulfoconjugation, lacked any demonstrable intrinsic affinity and/or efficacy on the dopaminergic and adrenergic receptors directly or indirectly (a) through their metabolic transformation or (b) through displacement of endogenous neurotransmitter.</abstract><cop>Philadelphia, PA</cop><cop>Hagerstown, MD</cop><pub>Lippincott-Raven Publishers</pub><pmid>2418311</pmid><doi>10.1097/00005344-198511000-00030</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record>
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source MEDLINE; Journals@Ovid LWW Legacy Archive; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Journals@Ovid Ovid Autoload
subjects Animals
Biological and medical sciences
Catecholaminergic system
Dogs
Dopamine - analogs & derivatives
Dopamine - metabolism
Dopamine - pharmacology
In Vitro Techniques
Male
Medical sciences
Muscle, Smooth, Vascular - drug effects
Muscle, Smooth, Vascular - metabolism
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Rats
Rats, Inbred Strains
Receptors, Adrenergic, alpha - metabolism
Receptors, Adrenergic, beta - metabolism
Receptors, Dopamine - drug effects
Receptors, Dopamine - metabolism
Splanchnic Circulation - drug effects
Sympathetic Nervous System - drug effects
title Adrenergic and Dopaminergic Properties of Dopamine Sulfoconjugates
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