JNJ-20788560 [9-(8-Azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic Acid Diethylamide], a Selective Delta Opioid Receptor Agonist, Is a Potent and Efficacious Antihyperalgesic Agent That Does Not Produce Respiratory Depression, Pharmacologic Tolerance, or Physical Dependence
μ-Opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple origins, but their side effects, such as constipation, respiratory depression, and abuse liability, adversely affect patients. The recent demonstration of the up-regulation and membrane targeting of the δ-opioi...
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| Veröffentlicht in: | The Journal of pharmacology and experimental therapeutics 2009-04, Vol.329 (1), p.241-251 |
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| creator | Codd, Ellen E. Carson, John R. Colburn, Raymond W. Stone, Dennis J. Van Besien, Christopher R. Zhang, Sui-Po Wade, Paul R. Gallantine, Elizabeth L. Meert, Theo F. Molino, Lory Pullan, Shirley Razler, Christine M. Dax, Scott L. Flores, Christopher M. |
| description | μ-Opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple origins, but their side effects, such as constipation, respiratory depression, and abuse liability, adversely affect patients. The recent demonstration of the up-regulation and membrane targeting of the δ-opioid receptor (DOR) following inflammation and the consequent enhanced therapeutic effect of δ-opioid agonists have enlivened the search for δ-opioid analgesic agents. JNJ-20788560 [9-(8-azabicyclo-[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide] had an affinity of 2.0 nM for DOR (rat brain cortex binding assay) and a naltrindole sensitive DOR potency of 5.6 nM (5′-O-(3-[35S]thio)triphosphate assay). The compound had a potency of 7.6 mg/kg p.o. in a rat zymosan radiant heat test and of 13.5 mg/kg p.o. in a rat Complete Freund’s adjuvant RH test but was virtually inactive in an uninflamed radiant heat test. In limited studies, tolerance was not observed to the antihyperalgesic or antinociceptive effects of the compound. Unlike ibuprofen, JNJ-20788560 did not produce gastrointestinal (GI) erosion. Although morphine reduced GI motility at all doses tested and reached nearly full effect at the highest dose, JNJ-20788560 did not retard transit at the lowest dose and reached only 11% reduction at the highest dose administered. Unlike morphine, JNJ-20788560 did not exhibit respiratory depression (blood gas analysis), and no withdrawal signs were precipitated by the administration of opioid (μ or δ) antagonists. Coupled with the previously published lack of self-administration behavior of the compound by alfentanil-trained primates, these findings strongly recommend δ-opioid agonists such as JNJ-20788560 for the relief of inflammatory hyperalgesia. |
| doi_str_mv | 10.1124/jpet.108.146969 |
| format | Article |
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The recent demonstration of the up-regulation and membrane targeting of the δ-opioid receptor (DOR) following inflammation and the consequent enhanced therapeutic effect of δ-opioid agonists have enlivened the search for δ-opioid analgesic agents. JNJ-20788560 [9-(8-azabicyclo-[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide] had an affinity of 2.0 nM for DOR (rat brain cortex binding assay) and a naltrindole sensitive DOR potency of 5.6 nM (5′-O-(3-[35S]thio)triphosphate assay). The compound had a potency of 7.6 mg/kg p.o. in a rat zymosan radiant heat test and of 13.5 mg/kg p.o. in a rat Complete Freund’s adjuvant RH test but was virtually inactive in an uninflamed radiant heat test. In limited studies, tolerance was not observed to the antihyperalgesic or antinociceptive effects of the compound. Unlike ibuprofen, JNJ-20788560 did not produce gastrointestinal (GI) erosion. Although morphine reduced GI motility at all doses tested and reached nearly full effect at the highest dose, JNJ-20788560 did not retard transit at the lowest dose and reached only 11% reduction at the highest dose administered. Unlike morphine, JNJ-20788560 did not exhibit respiratory depression (blood gas analysis), and no withdrawal signs were precipitated by the administration of opioid (μ or δ) antagonists. Coupled with the previously published lack of self-administration behavior of the compound by alfentanil-trained primates, these findings strongly recommend δ-opioid agonists such as JNJ-20788560 for the relief of inflammatory hyperalgesia.</description><identifier>ISSN: 0022-3565</identifier><identifier>EISSN: 1521-0103</identifier><identifier>DOI: 10.1124/jpet.108.146969</identifier><identifier>PMID: 19151246</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Alfentanil - pharmacology ; Analgesics, Opioid ; Animals ; Azabicyclo Compounds - adverse effects ; Azabicyclo Compounds - pharmacology ; Azabicyclo Compounds - toxicity ; Cricetinae ; Drug Tolerance ; Gastrointestinal Motility - drug effects ; Guanosine 5'-O-(3-Thiotriphosphate) - metabolism ; Hot Temperature ; Hyperalgesia - drug therapy ; Irritants - toxicity ; Male ; Mice ; Pain Measurement - drug effects ; Rats ; Rats, Wistar ; Receptors, Opioid, delta - agonists ; Receptors, Opioid, delta - metabolism ; Respiratory Insufficiency - chemically induced ; Respiratory Insufficiency - physiopathology ; Seizures - chemically induced ; Self Administration ; Stomach Ulcer - chemically induced ; Stomach Ulcer - pathology ; Substance Withdrawal Syndrome - psychology ; Substance-Related Disorders - physiopathology ; Xanthenes - adverse effects ; Xanthenes - pharmacology ; Xanthenes - toxicity ; Zymosan</subject><ispartof>The Journal of pharmacology and experimental therapeutics, 2009-04, Vol.329 (1), p.241-251</ispartof><rights>2009 American Society for Pharmacology and Experimental Therapeutics</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c330t-b771bc5019bb8abf9bfdee287f6d2cd64c4d4036472c1a68b84d29aad330f6373</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19151246$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Codd, Ellen E.</creatorcontrib><creatorcontrib>Carson, John R.</creatorcontrib><creatorcontrib>Colburn, Raymond W.</creatorcontrib><creatorcontrib>Stone, Dennis J.</creatorcontrib><creatorcontrib>Van Besien, Christopher R.</creatorcontrib><creatorcontrib>Zhang, Sui-Po</creatorcontrib><creatorcontrib>Wade, Paul R.</creatorcontrib><creatorcontrib>Gallantine, Elizabeth L.</creatorcontrib><creatorcontrib>Meert, Theo F.</creatorcontrib><creatorcontrib>Molino, Lory</creatorcontrib><creatorcontrib>Pullan, Shirley</creatorcontrib><creatorcontrib>Razler, Christine M.</creatorcontrib><creatorcontrib>Dax, Scott L.</creatorcontrib><creatorcontrib>Flores, Christopher M.</creatorcontrib><title>JNJ-20788560 [9-(8-Azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic Acid Diethylamide], a Selective Delta Opioid Receptor Agonist, Is a Potent and Efficacious Antihyperalgesic Agent That Does Not Produce Respiratory Depression, Pharmacologic Tolerance, or Physical Dependence</title><title>The Journal of pharmacology and experimental therapeutics</title><addtitle>J Pharmacol Exp Ther</addtitle><description>μ-Opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple origins, but their side effects, such as constipation, respiratory depression, and abuse liability, adversely affect patients. The recent demonstration of the up-regulation and membrane targeting of the δ-opioid receptor (DOR) following inflammation and the consequent enhanced therapeutic effect of δ-opioid agonists have enlivened the search for δ-opioid analgesic agents. JNJ-20788560 [9-(8-azabicyclo-[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide] had an affinity of 2.0 nM for DOR (rat brain cortex binding assay) and a naltrindole sensitive DOR potency of 5.6 nM (5′-O-(3-[35S]thio)triphosphate assay). The compound had a potency of 7.6 mg/kg p.o. in a rat zymosan radiant heat test and of 13.5 mg/kg p.o. in a rat Complete Freund’s adjuvant RH test but was virtually inactive in an uninflamed radiant heat test. In limited studies, tolerance was not observed to the antihyperalgesic or antinociceptive effects of the compound. Unlike ibuprofen, JNJ-20788560 did not produce gastrointestinal (GI) erosion. Although morphine reduced GI motility at all doses tested and reached nearly full effect at the highest dose, JNJ-20788560 did not retard transit at the lowest dose and reached only 11% reduction at the highest dose administered. Unlike morphine, JNJ-20788560 did not exhibit respiratory depression (blood gas analysis), and no withdrawal signs were precipitated by the administration of opioid (μ or δ) antagonists. Coupled with the previously published lack of self-administration behavior of the compound by alfentanil-trained primates, these findings strongly recommend δ-opioid agonists such as JNJ-20788560 for the relief of inflammatory hyperalgesia.</description><subject>Alfentanil - pharmacology</subject><subject>Analgesics, Opioid</subject><subject>Animals</subject><subject>Azabicyclo Compounds - adverse effects</subject><subject>Azabicyclo Compounds - pharmacology</subject><subject>Azabicyclo Compounds - toxicity</subject><subject>Cricetinae</subject><subject>Drug Tolerance</subject><subject>Gastrointestinal Motility - drug effects</subject><subject>Guanosine 5'-O-(3-Thiotriphosphate) - metabolism</subject><subject>Hot Temperature</subject><subject>Hyperalgesia - drug therapy</subject><subject>Irritants - toxicity</subject><subject>Male</subject><subject>Mice</subject><subject>Pain Measurement - drug effects</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Opioid, delta - agonists</subject><subject>Receptors, Opioid, delta - metabolism</subject><subject>Respiratory Insufficiency - chemically induced</subject><subject>Respiratory Insufficiency - physiopathology</subject><subject>Seizures - chemically induced</subject><subject>Self Administration</subject><subject>Stomach Ulcer - chemically induced</subject><subject>Stomach Ulcer - pathology</subject><subject>Substance Withdrawal Syndrome - psychology</subject><subject>Substance-Related Disorders - physiopathology</subject><subject>Xanthenes - adverse effects</subject><subject>Xanthenes - pharmacology</subject><subject>Xanthenes - toxicity</subject><subject>Zymosan</subject><issn>0022-3565</issn><issn>1521-0103</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kc9r2zAcxb2xsWbdzjsMhk5lgyjVD1u2j6Hp1pbShi07lWJk6etYxbGMpHT1_vrJpNDTTkLS573v9_GS5BMlC0pZevowQFhQUixoKkpRvk5mNGMUE0r4m2RGCGOYZyI7St57_0AITVPB3yVHtKRZlIvZq89XN1eYkbwoMkHQXYm_Fnj5V9ZGjaqzd3zBFvTeqoA5HjujoYdvuLzAT7IPbbzEZyVdbZ_ip0JLZTRaGQjt2MldpO_nSKJf0IEK5hHQCrog0e1gbOR-goIhWIeWW9sbH-bo0kd6bQP0Acleo_OmMUoqY_ceLftg2nEAJ7st-GnWdsI2rQxoZcGjGxvQ2lm9VxCt_WCcjOZjnDk48N7Yfo7WrXQ7qWxnt9FhY7to1yuYo7jFuh2jrewmAfQxqIIPydtGdh4-Pp_Hye_v55uzC3x9--PybHmNFeck4DrPaa0yQsu6LmTdlHWjAViRN0IzpUWqUp0SLtKcKSpFURepZqWUOqobwXN-nJwefJWz3jtoqsGZnXRjRUk11VxNNcdLUR1qjoovB8Wwr3egX_jnXiNwcgBas23_GAfV8JJ9rDgrK1qxlEawPIAQAz4acJVXZgqvo0iFSlvz3y3-AZi6xqw</recordid><startdate>200904</startdate><enddate>200904</enddate><creator>Codd, Ellen E.</creator><creator>Carson, John R.</creator><creator>Colburn, Raymond W.</creator><creator>Stone, Dennis J.</creator><creator>Van Besien, Christopher R.</creator><creator>Zhang, Sui-Po</creator><creator>Wade, Paul R.</creator><creator>Gallantine, Elizabeth L.</creator><creator>Meert, Theo F.</creator><creator>Molino, Lory</creator><creator>Pullan, Shirley</creator><creator>Razler, Christine M.</creator><creator>Dax, Scott L.</creator><creator>Flores, Christopher M.</creator><general>Elsevier Inc</general><general>American Society for Pharmacology and Experimental Therapeutics</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></search><sort><creationdate>200904</creationdate><title>JNJ-20788560 [9-(8-Azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic Acid Diethylamide], a Selective Delta Opioid Receptor Agonist, Is a Potent and Efficacious Antihyperalgesic Agent That Does Not Produce Respiratory Depression, Pharmacologic Tolerance, or Physical Dependence</title><author>Codd, Ellen E. ; Carson, John R. ; Colburn, Raymond W. ; Stone, Dennis J. ; Van Besien, Christopher R. ; Zhang, Sui-Po ; Wade, Paul R. ; Gallantine, Elizabeth L. ; Meert, Theo F. ; Molino, Lory ; Pullan, Shirley ; Razler, Christine M. ; Dax, Scott L. ; Flores, Christopher M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c330t-b771bc5019bb8abf9bfdee287f6d2cd64c4d4036472c1a68b84d29aad330f6373</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Alfentanil - pharmacology</topic><topic>Analgesics, Opioid</topic><topic>Animals</topic><topic>Azabicyclo Compounds - adverse effects</topic><topic>Azabicyclo Compounds - pharmacology</topic><topic>Azabicyclo Compounds - toxicity</topic><topic>Cricetinae</topic><topic>Drug Tolerance</topic><topic>Gastrointestinal Motility - drug effects</topic><topic>Guanosine 5'-O-(3-Thiotriphosphate) - metabolism</topic><topic>Hot Temperature</topic><topic>Hyperalgesia - drug therapy</topic><topic>Irritants - toxicity</topic><topic>Male</topic><topic>Mice</topic><topic>Pain Measurement - drug effects</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Opioid, delta - agonists</topic><topic>Receptors, Opioid, delta - metabolism</topic><topic>Respiratory Insufficiency - chemically induced</topic><topic>Respiratory Insufficiency - physiopathology</topic><topic>Seizures - chemically induced</topic><topic>Self Administration</topic><topic>Stomach Ulcer - chemically induced</topic><topic>Stomach Ulcer - pathology</topic><topic>Substance Withdrawal Syndrome - psychology</topic><topic>Substance-Related Disorders - physiopathology</topic><topic>Xanthenes - adverse effects</topic><topic>Xanthenes - pharmacology</topic><topic>Xanthenes - toxicity</topic><topic>Zymosan</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Codd, Ellen E.</creatorcontrib><creatorcontrib>Carson, John R.</creatorcontrib><creatorcontrib>Colburn, Raymond W.</creatorcontrib><creatorcontrib>Stone, Dennis J.</creatorcontrib><creatorcontrib>Van Besien, Christopher R.</creatorcontrib><creatorcontrib>Zhang, Sui-Po</creatorcontrib><creatorcontrib>Wade, Paul R.</creatorcontrib><creatorcontrib>Gallantine, Elizabeth L.</creatorcontrib><creatorcontrib>Meert, Theo F.</creatorcontrib><creatorcontrib>Molino, Lory</creatorcontrib><creatorcontrib>Pullan, Shirley</creatorcontrib><creatorcontrib>Razler, Christine M.</creatorcontrib><creatorcontrib>Dax, Scott L.</creatorcontrib><creatorcontrib>Flores, Christopher M.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>The Journal of pharmacology and experimental therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Codd, Ellen E.</au><au>Carson, John R.</au><au>Colburn, Raymond W.</au><au>Stone, Dennis J.</au><au>Van Besien, Christopher R.</au><au>Zhang, Sui-Po</au><au>Wade, Paul R.</au><au>Gallantine, Elizabeth L.</au><au>Meert, Theo F.</au><au>Molino, Lory</au><au>Pullan, Shirley</au><au>Razler, Christine M.</au><au>Dax, Scott L.</au><au>Flores, Christopher M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>JNJ-20788560 [9-(8-Azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic Acid Diethylamide], a Selective Delta Opioid Receptor Agonist, Is a Potent and Efficacious Antihyperalgesic Agent That Does Not Produce Respiratory Depression, Pharmacologic Tolerance, or Physical Dependence</atitle><jtitle>The Journal of pharmacology and experimental therapeutics</jtitle><addtitle>J Pharmacol Exp Ther</addtitle><date>2009-04</date><risdate>2009</risdate><volume>329</volume><issue>1</issue><spage>241</spage><epage>251</epage><pages>241-251</pages><issn>0022-3565</issn><eissn>1521-0103</eissn><abstract>μ-Opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple origins, but their side effects, such as constipation, respiratory depression, and abuse liability, adversely affect patients. The recent demonstration of the up-regulation and membrane targeting of the δ-opioid receptor (DOR) following inflammation and the consequent enhanced therapeutic effect of δ-opioid agonists have enlivened the search for δ-opioid analgesic agents. JNJ-20788560 [9-(8-azabicyclo-[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide] had an affinity of 2.0 nM for DOR (rat brain cortex binding assay) and a naltrindole sensitive DOR potency of 5.6 nM (5′-O-(3-[35S]thio)triphosphate assay). The compound had a potency of 7.6 mg/kg p.o. in a rat zymosan radiant heat test and of 13.5 mg/kg p.o. in a rat Complete Freund’s adjuvant RH test but was virtually inactive in an uninflamed radiant heat test. In limited studies, tolerance was not observed to the antihyperalgesic or antinociceptive effects of the compound. Unlike ibuprofen, JNJ-20788560 did not produce gastrointestinal (GI) erosion. Although morphine reduced GI motility at all doses tested and reached nearly full effect at the highest dose, JNJ-20788560 did not retard transit at the lowest dose and reached only 11% reduction at the highest dose administered. Unlike morphine, JNJ-20788560 did not exhibit respiratory depression (blood gas analysis), and no withdrawal signs were precipitated by the administration of opioid (μ or δ) antagonists. Coupled with the previously published lack of self-administration behavior of the compound by alfentanil-trained primates, these findings strongly recommend δ-opioid agonists such as JNJ-20788560 for the relief of inflammatory hyperalgesia.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>19151246</pmid><doi>10.1124/jpet.108.146969</doi><tpages>11</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | The Journal of pharmacology and experimental therapeutics, 2009-04, Vol.329 (1), p.241-251 |
| issn | 0022-3565 1521-0103 |
| language | eng |
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| source | MEDLINE; Alma/SFX Local Collection |
| subjects | Alfentanil - pharmacology Analgesics, Opioid Animals Azabicyclo Compounds - adverse effects Azabicyclo Compounds - pharmacology Azabicyclo Compounds - toxicity Cricetinae Drug Tolerance Gastrointestinal Motility - drug effects Guanosine 5'-O-(3-Thiotriphosphate) - metabolism Hot Temperature Hyperalgesia - drug therapy Irritants - toxicity Male Mice Pain Measurement - drug effects Rats Rats, Wistar Receptors, Opioid, delta - agonists Receptors, Opioid, delta - metabolism Respiratory Insufficiency - chemically induced Respiratory Insufficiency - physiopathology Seizures - chemically induced Self Administration Stomach Ulcer - chemically induced Stomach Ulcer - pathology Substance Withdrawal Syndrome - psychology Substance-Related Disorders - physiopathology Xanthenes - adverse effects Xanthenes - pharmacology Xanthenes - toxicity Zymosan |
| title | JNJ-20788560 [9-(8-Azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic Acid Diethylamide], a Selective Delta Opioid Receptor Agonist, Is a Potent and Efficacious Antihyperalgesic Agent That Does Not Produce Respiratory Depression, Pharmacologic Tolerance, or Physical Dependence |
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