Study of μ- and δ-Opioid Activities in Agents with Various κ-Receptor Selectivity
A putative opioid agonist RU-1205 was ineffective within in vitro model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC 50 =2.6×10 —7 M. In vivo...
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| Veröffentlicht in: | Bulletin of experimental biology and medicine 2017-03, Vol.162 (5), p.632-635 |
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| container_title | Bulletin of experimental biology and medicine |
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| creator | Grechko, O. Yu Litvinov, R. A. Spasov, A. A. Rashchenko, A. I. Shtareva, D. M. Anisimova, V. A. Minkin, V. I. |
| description | A putative opioid agonist RU-1205 was ineffective within
in vitro
model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC
50
=2.6×10
—7
M.
In vivo
experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77.1% (1 mg/kg) and by 45.5% (10 mg/kg). Morphine-induced inhibition of peristalsis was dose-dependent with maximum effect (by 68.6%) observed in the dose of 10 mg/kg. It was concluded that the effects of RU-1205 are not related to activation μ- and δ-opioid receptors known to mediate the effects of non-selective opioid agonist morphine and agonist-antagonist butorphanol. |
| doi_str_mv | 10.1007/s10517-017-3674-5 |
| format | Article |
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in vitro
model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC
50
=2.6×10
—7
M.
In vivo
experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77.1% (1 mg/kg) and by 45.5% (10 mg/kg). Morphine-induced inhibition of peristalsis was dose-dependent with maximum effect (by 68.6%) observed in the dose of 10 mg/kg. It was concluded that the effects of RU-1205 are not related to activation μ- and δ-opioid receptors known to mediate the effects of non-selective opioid agonist morphine and agonist-antagonist butorphanol.</description><identifier>ISSN: 0007-4888</identifier><identifier>EISSN: 1573-8221</identifier><identifier>DOI: 10.1007/s10517-017-3674-5</identifier><identifier>PMID: 28361412</identifier><language>eng</language><publisher>New York: Springer US</publisher><subject>Analgesics, Opioid - pharmacology ; Animals ; Benzimidazoles - pharmacology ; Biomedical and Life Sciences ; Biomedicine ; Butorphanol - pharmacology ; Cell Biology ; Drug Evaluation, Preclinical ; Gastrointestinal Motility - drug effects ; Ileum - drug effects ; Ileum - physiology ; Internal Medicine ; Laboratory Medicine ; Male ; Morphine - pharmacology ; Morpholines - pharmacology ; Narcotic Antagonists - pharmacology ; Pathology ; Pharmacology and Toxicology ; Rats ; Receptors, Opioid, kappa - physiology</subject><ispartof>Bulletin of experimental biology and medicine, 2017-03, Vol.162 (5), p.632-635</ispartof><rights>Springer Science+Business Media New York 2017</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c377t-c88bb817dd3b8f29b9d0e3c5cd778b84446970055f2b088147bfe50dc47671173</citedby><cites>FETCH-LOGICAL-c377t-c88bb817dd3b8f29b9d0e3c5cd778b84446970055f2b088147bfe50dc47671173</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10517-017-3674-5$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10517-017-3674-5$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,778,782,27911,27912,41475,42544,51306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28361412$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Grechko, O. Yu</creatorcontrib><creatorcontrib>Litvinov, R. A.</creatorcontrib><creatorcontrib>Spasov, A. A.</creatorcontrib><creatorcontrib>Rashchenko, A. I.</creatorcontrib><creatorcontrib>Shtareva, D. M.</creatorcontrib><creatorcontrib>Anisimova, V. A.</creatorcontrib><creatorcontrib>Minkin, V. I.</creatorcontrib><title>Study of μ- and δ-Opioid Activities in Agents with Various κ-Receptor Selectivity</title><title>Bulletin of experimental biology and medicine</title><addtitle>Bull Exp Biol Med</addtitle><addtitle>Bull Exp Biol Med</addtitle><description>A putative opioid agonist RU-1205 was ineffective within
in vitro
model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC
50
=2.6×10
—7
M.
In vivo
experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77.1% (1 mg/kg) and by 45.5% (10 mg/kg). Morphine-induced inhibition of peristalsis was dose-dependent with maximum effect (by 68.6%) observed in the dose of 10 mg/kg. It was concluded that the effects of RU-1205 are not related to activation μ- and δ-opioid receptors known to mediate the effects of non-selective opioid agonist morphine and agonist-antagonist butorphanol.</description><subject>Analgesics, Opioid - pharmacology</subject><subject>Animals</subject><subject>Benzimidazoles - pharmacology</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Butorphanol - pharmacology</subject><subject>Cell Biology</subject><subject>Drug Evaluation, Preclinical</subject><subject>Gastrointestinal Motility - drug effects</subject><subject>Ileum - drug effects</subject><subject>Ileum - physiology</subject><subject>Internal Medicine</subject><subject>Laboratory Medicine</subject><subject>Male</subject><subject>Morphine - pharmacology</subject><subject>Morpholines - pharmacology</subject><subject>Narcotic Antagonists - pharmacology</subject><subject>Pathology</subject><subject>Pharmacology and Toxicology</subject><subject>Rats</subject><subject>Receptors, Opioid, kappa - physiology</subject><issn>0007-4888</issn><issn>1573-8221</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkMtKxDAUhoMoOl4ewI1k6Saa0zTN6XIQbyAI3rahTdIxMtOOSavMe7kSn2GeyQ4dXYqLQzjk-38OHyGHwE-Ac3UagUtQjPcjMpUyuUFGIJVgmCSwSUa8h1iKiDtkN8aX1coz2CY7CYoMUkhG5OG-7eyCNhVdfjFa1JYuP9jt3Dfe0rFp_ZtvvYvU13Q8cXUb6btvn-lTEXzTRbr8ZHfOuHnbBHrvpm4ILPbJVlVMoztYv3vk8eL84eyK3dxeXp-Nb5gRSrXMIJYlgrJWlFgleZlb7oSRxiqFJaZpmuWKcymrpOSIkKqycpJbk6pMASixR46H3nloXjsXWz3z0bjptKhdf54GzJXIQXL8B4oCEKRYoTCgJjQxBlfpefCzIiw0cL3yrgfvuveuV9617DNH6_qunDn7m_gR3QPJAMT-q564oF-aLtS9nT9avwHI644H</recordid><startdate>20170301</startdate><enddate>20170301</enddate><creator>Grechko, O. Yu</creator><creator>Litvinov, R. A.</creator><creator>Spasov, A. A.</creator><creator>Rashchenko, A. I.</creator><creator>Shtareva, D. M.</creator><creator>Anisimova, V. A.</creator><creator>Minkin, V. I.</creator><general>Springer US</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>7X8</scope><scope>7U7</scope><scope>C1K</scope></search><sort><creationdate>20170301</creationdate><title>Study of μ- and δ-Opioid Activities in Agents with Various κ-Receptor Selectivity</title><author>Grechko, O. Yu ; Litvinov, R. A. ; Spasov, A. A. ; Rashchenko, A. I. ; Shtareva, D. M. ; Anisimova, V. A. ; Minkin, V. 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Yu</creatorcontrib><creatorcontrib>Litvinov, R. A.</creatorcontrib><creatorcontrib>Spasov, A. A.</creatorcontrib><creatorcontrib>Rashchenko, A. I.</creatorcontrib><creatorcontrib>Shtareva, D. M.</creatorcontrib><creatorcontrib>Anisimova, V. A.</creatorcontrib><creatorcontrib>Minkin, V. I.</creatorcontrib><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><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><jtitle>Bulletin of experimental biology and medicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Grechko, O. Yu</au><au>Litvinov, R. A.</au><au>Spasov, A. A.</au><au>Rashchenko, A. I.</au><au>Shtareva, D. 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in vitro
model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC
50
=2.6×10
—7
M.
In vivo
experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77.1% (1 mg/kg) and by 45.5% (10 mg/kg). Morphine-induced inhibition of peristalsis was dose-dependent with maximum effect (by 68.6%) observed in the dose of 10 mg/kg. It was concluded that the effects of RU-1205 are not related to activation μ- and δ-opioid receptors known to mediate the effects of non-selective opioid agonist morphine and agonist-antagonist butorphanol.</abstract><cop>New York</cop><pub>Springer US</pub><pmid>28361412</pmid><doi>10.1007/s10517-017-3674-5</doi><tpages>4</tpages></addata></record> |
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| ispartof | Bulletin of experimental biology and medicine, 2017-03, Vol.162 (5), p.632-635 |
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| subjects | Analgesics, Opioid - pharmacology Animals Benzimidazoles - pharmacology Biomedical and Life Sciences Biomedicine Butorphanol - pharmacology Cell Biology Drug Evaluation, Preclinical Gastrointestinal Motility - drug effects Ileum - drug effects Ileum - physiology Internal Medicine Laboratory Medicine Male Morphine - pharmacology Morpholines - pharmacology Narcotic Antagonists - pharmacology Pathology Pharmacology and Toxicology Rats Receptors, Opioid, kappa - physiology |
| title | Study of μ- and δ-Opioid Activities in Agents with Various κ-Receptor Selectivity |
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