Electrophysiological and behavioral effects of Tyr- d-Arg-Phe-Sar on locus coeruleus neurons of the rat
The effect of Tyr- d-Arg-Phe-Sar (TAPS), a μ-selective tetrapeptide analog of dermorphin, was studied in the rat both in vitro, using slices of the locus coeruleus, and in vivo, after microinjection into the locus coeruleus. In electrophysiological studies, TAPS (1–100 nM) was able to inhibit sponta...
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| Veröffentlicht in: | European journal of pharmacology 1998-06, Vol.351 (1), p.23-30 |
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| creator | Yang, Yea-Ru Lee, Eminy H.Y Chiu, Tsai-Hsien |
| description | The effect of Tyr-
d-Arg-Phe-Sar (TAPS), a
μ-selective tetrapeptide analog of dermorphin, was studied in the rat both in vitro, using slices of the locus coeruleus, and in vivo, after microinjection into the locus coeruleus. In electrophysiological studies, TAPS (1–100 nM) was able to inhibit spontaneous firing, cause hyperpolarization of the membrane potential and reduce the input resistance of neurons of the locus coeruleus, suggesting that there was an effect on the potassium channels. Based on the inhibition of the spontaneous firing rate, the average IC
50 for TAPS was calculated to be 1.9 nM, a value lower than that reported for dermorphin or morphine. The TAPS-induced effects were antagonized by naloxone, with a dissociation equilibrium constant of 1.96±0.14 nM. The results indicate that TAPS binds to
μ-opioid receptors on the cell membrane of neurons of the locus coeruleus to cause its inhibitory actions. In behavioral study, TAPS was microinjected bilaterally via chronically implanted cannulae into the locus coeruleus of non-anesthetized rats and its effects on locomotor activity determined. TAPS, at concentrations of 1
μM and 10
μM, but not of 0.1
μM, induced hypolocomotion/sedation and the effect was significantly reversed by naloxone (5 mg/kg i.p.). Taken together, these data suggest that TAPS has an inhibitory effect on neurons of the locus coeruleus and produces hypolocomotive/sedative effects in vivo. |
| doi_str_mv | 10.1016/S0014-2999(98)00296-9 |
| format | Article |
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d-Arg-Phe-Sar (TAPS), a
μ-selective tetrapeptide analog of dermorphin, was studied in the rat both in vitro, using slices of the locus coeruleus, and in vivo, after microinjection into the locus coeruleus. In electrophysiological studies, TAPS (1–100 nM) was able to inhibit spontaneous firing, cause hyperpolarization of the membrane potential and reduce the input resistance of neurons of the locus coeruleus, suggesting that there was an effect on the potassium channels. Based on the inhibition of the spontaneous firing rate, the average IC
50 for TAPS was calculated to be 1.9 nM, a value lower than that reported for dermorphin or morphine. The TAPS-induced effects were antagonized by naloxone, with a dissociation equilibrium constant of 1.96±0.14 nM. The results indicate that TAPS binds to
μ-opioid receptors on the cell membrane of neurons of the locus coeruleus to cause its inhibitory actions. In behavioral study, TAPS was microinjected bilaterally via chronically implanted cannulae into the locus coeruleus of non-anesthetized rats and its effects on locomotor activity determined. TAPS, at concentrations of 1
μM and 10
μM, but not of 0.1
μM, induced hypolocomotion/sedation and the effect was significantly reversed by naloxone (5 mg/kg i.p.). Taken together, these data suggest that TAPS has an inhibitory effect on neurons of the locus coeruleus and produces hypolocomotive/sedative effects in vivo.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/S0014-2999(98)00296-9</identifier><identifier>PMID: 9698201</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Analgesics - administration & dosage ; Analgesics - pharmacology ; Animals ; Biological and medical sciences ; Dose-Response Relationship, Drug ; Electrophysiology ; Hypnotics and Sedatives - pharmacology ; Injections, Intraventricular ; Intracellular recording ; Locomotor activity ; Locus coeruleus ; Locus Coeruleus - drug effects ; Male ; Medical sciences ; Membrane Potentials - drug effects ; Motor Activity - drug effects ; Neurons - drug effects ; Neurons - physiology ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Oligopeptides - administration & dosage ; Oligopeptides - antagonists & inhibitors ; Oligopeptides - pharmacology ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pharmacology. Drug treatments ; Potassium Channels - drug effects ; Rats ; Rats, Sprague-Dawley ; Receptors, Opioid, mu - drug effects ; Receptors, Opioid, mu - metabolism ; Tyr- d-Arg-Phe-Sar</subject><ispartof>European journal of pharmacology, 1998-06, Vol.351 (1), p.23-30</ispartof><rights>1998 Elsevier Science B.V.</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c455t-7c9736bfd3e42c70246a47a0bdbeca0bc85a9a29255fae34edfe852a5d7309163</citedby><cites>FETCH-LOGICAL-c455t-7c9736bfd3e42c70246a47a0bdbeca0bc85a9a29255fae34edfe852a5d7309163</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0014299998002969$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2379978$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9698201$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yang, Yea-Ru</creatorcontrib><creatorcontrib>Lee, Eminy H.Y</creatorcontrib><creatorcontrib>Chiu, Tsai-Hsien</creatorcontrib><title>Electrophysiological and behavioral effects of Tyr- d-Arg-Phe-Sar on locus coeruleus neurons of the rat</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The effect of Tyr-
d-Arg-Phe-Sar (TAPS), a
μ-selective tetrapeptide analog of dermorphin, was studied in the rat both in vitro, using slices of the locus coeruleus, and in vivo, after microinjection into the locus coeruleus. In electrophysiological studies, TAPS (1–100 nM) was able to inhibit spontaneous firing, cause hyperpolarization of the membrane potential and reduce the input resistance of neurons of the locus coeruleus, suggesting that there was an effect on the potassium channels. Based on the inhibition of the spontaneous firing rate, the average IC
50 for TAPS was calculated to be 1.9 nM, a value lower than that reported for dermorphin or morphine. The TAPS-induced effects were antagonized by naloxone, with a dissociation equilibrium constant of 1.96±0.14 nM. The results indicate that TAPS binds to
μ-opioid receptors on the cell membrane of neurons of the locus coeruleus to cause its inhibitory actions. In behavioral study, TAPS was microinjected bilaterally via chronically implanted cannulae into the locus coeruleus of non-anesthetized rats and its effects on locomotor activity determined. TAPS, at concentrations of 1
μM and 10
μM, but not of 0.1
μM, induced hypolocomotion/sedation and the effect was significantly reversed by naloxone (5 mg/kg i.p.). Taken together, these data suggest that TAPS has an inhibitory effect on neurons of the locus coeruleus and produces hypolocomotive/sedative effects in vivo.</description><subject>Analgesics - administration & dosage</subject><subject>Analgesics - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Dose-Response Relationship, Drug</subject><subject>Electrophysiology</subject><subject>Hypnotics and Sedatives - pharmacology</subject><subject>Injections, Intraventricular</subject><subject>Intracellular recording</subject><subject>Locomotor activity</subject><subject>Locus coeruleus</subject><subject>Locus Coeruleus - drug effects</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Membrane Potentials - drug effects</subject><subject>Motor Activity - drug effects</subject><subject>Neurons - drug effects</subject><subject>Neurons - physiology</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Oligopeptides - administration & dosage</subject><subject>Oligopeptides - antagonists & inhibitors</subject><subject>Oligopeptides - pharmacology</subject><subject>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</subject><subject>Pharmacology. Drug treatments</subject><subject>Potassium Channels - drug effects</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, Opioid, mu - drug effects</subject><subject>Receptors, Opioid, mu - metabolism</subject><subject>Tyr- d-Arg-Phe-Sar</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkF1rHCEUhiU0pJu0PyHgRSnJhak646hXJYT0AwIJJL0WR4-7htlxqzOB_fc1u8ve9uocOc-rngehS0ZvGGXdt2dKWUu41vpKq2tKue6IPkELpqQmVDL-AS2OyEd0XsorpVRoLs7Qme604pQt0PJ-ADfltFltS0xDWkZnB2xHj3tY2beYcj1CCBUqOAX8ss0Ee3Kbl-RpBeTZZpxGPCQ3F-wS5HmA2o0w5zTuAtMKcLbTJ3Qa7FDg86FeoD8_7l_ufpGHx5-_724fiGuFmIh0WjZdH3wDLXeS8razrbS09z24WpwSVltelxDBQtOCD6AEt8LLhmrWNRfo6_7eTU5_ZyiTWcfiYBjsCGkuRlUFSrWsgmIPupxKyRDMJse1zVvDqHkXbHaCzbs9o5XZCTa65i4PD8z9GvwxdTBa518Oc1uqypDt6GI5YryRWktVse97DKqMtwjZFBdhdOBjrq6NT_E_H_kHnJqYWw</recordid><startdate>19980612</startdate><enddate>19980612</enddate><creator>Yang, Yea-Ru</creator><creator>Lee, Eminy H.Y</creator><creator>Chiu, Tsai-Hsien</creator><general>Elsevier B.V</general><general>Elsevier</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>19980612</creationdate><title>Electrophysiological and behavioral effects of Tyr- d-Arg-Phe-Sar on locus coeruleus neurons of the rat</title><author>Yang, Yea-Ru ; Lee, Eminy H.Y ; Chiu, Tsai-Hsien</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c455t-7c9736bfd3e42c70246a47a0bdbeca0bc85a9a29255fae34edfe852a5d7309163</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Analgesics - administration & dosage</topic><topic>Analgesics - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Dose-Response Relationship, Drug</topic><topic>Electrophysiology</topic><topic>Hypnotics and Sedatives - pharmacology</topic><topic>Injections, Intraventricular</topic><topic>Intracellular recording</topic><topic>Locomotor activity</topic><topic>Locus coeruleus</topic><topic>Locus Coeruleus - drug effects</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Membrane Potentials - drug effects</topic><topic>Motor Activity - drug effects</topic><topic>Neurons - drug effects</topic><topic>Neurons - physiology</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Oligopeptides - administration & dosage</topic><topic>Oligopeptides - antagonists & inhibitors</topic><topic>Oligopeptides - pharmacology</topic><topic>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</topic><topic>Pharmacology. Drug treatments</topic><topic>Potassium Channels - drug effects</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, Opioid, mu - drug effects</topic><topic>Receptors, Opioid, mu - metabolism</topic><topic>Tyr- d-Arg-Phe-Sar</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yang, Yea-Ru</creatorcontrib><creatorcontrib>Lee, Eminy H.Y</creatorcontrib><creatorcontrib>Chiu, Tsai-Hsien</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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yang, Yea-Ru</au><au>Lee, Eminy H.Y</au><au>Chiu, Tsai-Hsien</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Electrophysiological and behavioral effects of Tyr- d-Arg-Phe-Sar on locus coeruleus neurons of the rat</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1998-06-12</date><risdate>1998</risdate><volume>351</volume><issue>1</issue><spage>23</spage><epage>30</epage><pages>23-30</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The effect of Tyr-
d-Arg-Phe-Sar (TAPS), a
μ-selective tetrapeptide analog of dermorphin, was studied in the rat both in vitro, using slices of the locus coeruleus, and in vivo, after microinjection into the locus coeruleus. In electrophysiological studies, TAPS (1–100 nM) was able to inhibit spontaneous firing, cause hyperpolarization of the membrane potential and reduce the input resistance of neurons of the locus coeruleus, suggesting that there was an effect on the potassium channels. Based on the inhibition of the spontaneous firing rate, the average IC
50 for TAPS was calculated to be 1.9 nM, a value lower than that reported for dermorphin or morphine. The TAPS-induced effects were antagonized by naloxone, with a dissociation equilibrium constant of 1.96±0.14 nM. The results indicate that TAPS binds to
μ-opioid receptors on the cell membrane of neurons of the locus coeruleus to cause its inhibitory actions. In behavioral study, TAPS was microinjected bilaterally via chronically implanted cannulae into the locus coeruleus of non-anesthetized rats and its effects on locomotor activity determined. TAPS, at concentrations of 1
μM and 10
μM, but not of 0.1
μM, induced hypolocomotion/sedation and the effect was significantly reversed by naloxone (5 mg/kg i.p.). Taken together, these data suggest that TAPS has an inhibitory effect on neurons of the locus coeruleus and produces hypolocomotive/sedative effects in vivo.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>9698201</pmid><doi>10.1016/S0014-2999(98)00296-9</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | European journal of pharmacology, 1998-06, Vol.351 (1), p.23-30 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| subjects | Analgesics - administration & dosage Analgesics - pharmacology Animals Biological and medical sciences Dose-Response Relationship, Drug Electrophysiology Hypnotics and Sedatives - pharmacology Injections, Intraventricular Intracellular recording Locomotor activity Locus coeruleus Locus Coeruleus - drug effects Male Medical sciences Membrane Potentials - drug effects Motor Activity - drug effects Neurons - drug effects Neurons - physiology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oligopeptides - administration & dosage Oligopeptides - antagonists & inhibitors Oligopeptides - pharmacology Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Potassium Channels - drug effects Rats Rats, Sprague-Dawley Receptors, Opioid, mu - drug effects Receptors, Opioid, mu - metabolism Tyr- d-Arg-Phe-Sar |
| title | Electrophysiological and behavioral effects of Tyr- d-Arg-Phe-Sar on locus coeruleus neurons of the rat |
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