The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions
Nociceptin/orphanin FQ (N/OFQ), the endogenous NOP receptor ligand, centrally modulates gastric motor and secretory functions and prevents ethanol-induced gastric lesions in rats. A recently synthesized N/OFQ analog, [(pF)Phe 4Aib 7Arg 14Lys 15]N/OFQ-NH 2 (UFP-112), acts as a highly potent and selec...
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| Veröffentlicht in: | Peptides (New York, N.Y. : 1980) N.Y. : 1980), 2007-10, Vol.28 (10), p.1974-1981 |
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| container_issue | 10 |
| container_start_page | 1974 |
| container_title | Peptides (New York, N.Y. : 1980) |
| container_volume | 28 |
| creator | Broccardo, M. Guerrini, R. Morini, G. Polidori, C. Agostini, S. Petrella, C. Improta, G. |
| description | Nociceptin/orphanin FQ (N/OFQ), the endogenous NOP receptor ligand, centrally modulates gastric motor and secretory functions and prevents ethanol-induced gastric lesions in rats. A recently synthesized N/OFQ analog, [(pF)Phe
4Aib
7Arg
14Lys
15]N/OFQ-NH
2 (UFP-112), acts as a highly potent and selective peptide agonist for NOP receptors and produces longer-lasting
in vitro and
in vivo effects in mice than the natural ligand N/OFQ. In this study, we evaluated the effects of centrally (intracerebroventricularly/icv) and peripherally (intraperitoneally/ip) injected UFP-112 on gastric emptying and gastric acid secretion, and on the development of gastric mucosal lesions induced by 50% ethanol in the rat. When injected icv, it dose-dependently delayed gastric emptying of a phenol red meal (by up to 70%), decreased gastric secretion in water-loaded rats after 90 pylorus ligature, and reduced ethanol-induced gastric lesions (by up to 87%). In all three assays, UFP-112 was more effective than N/OFQ. The highly selective NOP receptor antagonist, UFP-101, decreased the efficacy of UFP-112, thus confirming that central NOP receptors mediate inhibitory control on these functional and pathological conditions in rats. Ip injected N/OFQ and UFP-112 induced non-dose-related gastric hypersecretory and antiulcer effects, which UFP-101 partially abolished. Ip N/OFQ appeared equiactive but about 30–100 times less potent than ip UFP-112 in stimulating gastric acid secretion and preventing lesion formation. When ip injected, both UFP-112 and N/OFQ left gastric emptying in rats unchanged, suggesting that peripheral NOP receptors have a role in mediating gastric hypersecretory and antiulcer effects but are not involved in regulating gastric motility. In addition, the inhibitory effects induced by this novel NOP receptor agonist lasted longer than those induced by N/OFQ. In conclusion, UFP-112 is a promising new pharmacological tool for studying the functional roles of the central and peripheral N/OFQ receptor system. |
| doi_str_mv | 10.1016/j.peptides.2007.07.021 |
| format | Article |
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4Aib
7Arg
14Lys
15]N/OFQ-NH
2 (UFP-112), acts as a highly potent and selective peptide agonist for NOP receptors and produces longer-lasting
in vitro and
in vivo effects in mice than the natural ligand N/OFQ. In this study, we evaluated the effects of centrally (intracerebroventricularly/icv) and peripherally (intraperitoneally/ip) injected UFP-112 on gastric emptying and gastric acid secretion, and on the development of gastric mucosal lesions induced by 50% ethanol in the rat. When injected icv, it dose-dependently delayed gastric emptying of a phenol red meal (by up to 70%), decreased gastric secretion in water-loaded rats after 90 pylorus ligature, and reduced ethanol-induced gastric lesions (by up to 87%). In all three assays, UFP-112 was more effective than N/OFQ. The highly selective NOP receptor antagonist, UFP-101, decreased the efficacy of UFP-112, thus confirming that central NOP receptors mediate inhibitory control on these functional and pathological conditions in rats. Ip injected N/OFQ and UFP-112 induced non-dose-related gastric hypersecretory and antiulcer effects, which UFP-101 partially abolished. Ip N/OFQ appeared equiactive but about 30–100 times less potent than ip UFP-112 in stimulating gastric acid secretion and preventing lesion formation. When ip injected, both UFP-112 and N/OFQ left gastric emptying in rats unchanged, suggesting that peripheral NOP receptors have a role in mediating gastric hypersecretory and antiulcer effects but are not involved in regulating gastric motility. In addition, the inhibitory effects induced by this novel NOP receptor agonist lasted longer than those induced by N/OFQ. In conclusion, UFP-112 is a promising new pharmacological tool for studying the functional roles of the central and peripheral N/OFQ receptor system.</description><identifier>ISSN: 0196-9781</identifier><identifier>EISSN: 1873-5169</identifier><identifier>DOI: 10.1016/j.peptides.2007.07.021</identifier><identifier>PMID: 17765363</identifier><identifier>CODEN: PPTDD5</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Animals ; Biological and medical sciences ; Fundamental and applied biological sciences. Psychology ; Gastric emptying ; Gastric Emptying - drug effects ; Opioid Peptides - pharmacology ; Rats ; Receptors, Opioid - agonists ; Secretion and ulcers ; Stomach - drug effects ; UFP-112 ; Vertebrates: endocrinology</subject><ispartof>Peptides (New York, N.Y. : 1980), 2007-10, Vol.28 (10), p.1974-1981</ispartof><rights>2007 Elsevier Inc.</rights><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c421t-5db90a678eee0eab9296ba4d225135fdc9e1c967f410acc25b97c67eeb2f26703</citedby><cites>FETCH-LOGICAL-c421t-5db90a678eee0eab9296ba4d225135fdc9e1c967f410acc25b97c67eeb2f26703</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.peptides.2007.07.021$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19126886$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17765363$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Broccardo, M.</creatorcontrib><creatorcontrib>Guerrini, R.</creatorcontrib><creatorcontrib>Morini, G.</creatorcontrib><creatorcontrib>Polidori, C.</creatorcontrib><creatorcontrib>Agostini, S.</creatorcontrib><creatorcontrib>Petrella, C.</creatorcontrib><creatorcontrib>Improta, G.</creatorcontrib><title>The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions</title><title>Peptides (New York, N.Y. : 1980)</title><addtitle>Peptides</addtitle><description>Nociceptin/orphanin FQ (N/OFQ), the endogenous NOP receptor ligand, centrally modulates gastric motor and secretory functions and prevents ethanol-induced gastric lesions in rats. A recently synthesized N/OFQ analog, [(pF)Phe
4Aib
7Arg
14Lys
15]N/OFQ-NH
2 (UFP-112), acts as a highly potent and selective peptide agonist for NOP receptors and produces longer-lasting
in vitro and
in vivo effects in mice than the natural ligand N/OFQ. In this study, we evaluated the effects of centrally (intracerebroventricularly/icv) and peripherally (intraperitoneally/ip) injected UFP-112 on gastric emptying and gastric acid secretion, and on the development of gastric mucosal lesions induced by 50% ethanol in the rat. When injected icv, it dose-dependently delayed gastric emptying of a phenol red meal (by up to 70%), decreased gastric secretion in water-loaded rats after 90 pylorus ligature, and reduced ethanol-induced gastric lesions (by up to 87%). In all three assays, UFP-112 was more effective than N/OFQ. The highly selective NOP receptor antagonist, UFP-101, decreased the efficacy of UFP-112, thus confirming that central NOP receptors mediate inhibitory control on these functional and pathological conditions in rats. Ip injected N/OFQ and UFP-112 induced non-dose-related gastric hypersecretory and antiulcer effects, which UFP-101 partially abolished. Ip N/OFQ appeared equiactive but about 30–100 times less potent than ip UFP-112 in stimulating gastric acid secretion and preventing lesion formation. When ip injected, both UFP-112 and N/OFQ left gastric emptying in rats unchanged, suggesting that peripheral NOP receptors have a role in mediating gastric hypersecretory and antiulcer effects but are not involved in regulating gastric motility. In addition, the inhibitory effects induced by this novel NOP receptor agonist lasted longer than those induced by N/OFQ. In conclusion, UFP-112 is a promising new pharmacological tool for studying the functional roles of the central and peripheral N/OFQ receptor system.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Gastric emptying</subject><subject>Gastric Emptying - drug effects</subject><subject>Opioid Peptides - pharmacology</subject><subject>Rats</subject><subject>Receptors, Opioid - agonists</subject><subject>Secretion and ulcers</subject><subject>Stomach - drug effects</subject><subject>UFP-112</subject><subject>Vertebrates: endocrinology</subject><issn>0196-9781</issn><issn>1873-5169</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1v1DAQhi0EokvhL1S-wKnZepzEjm-gikKlSnBoz5ZjT3a9ytrB9hb670m0Cz1WGmmkV8986CHkAtgaGIir3XrCqXiHec0Zk-ulOLwiK-hkXbUg1GuyYqBEpWQHZ-RdzjvGWNOo7i05AylFW4t6Rf7cb5FuTC7JW4rDgLZkGgf6cPOzAuCX1NCAv2mI1tvlYLiKadqa4ANNuCQxUbOJwedySedw2j5lH8e48daM1ARHJ1O2_wMbg_PFx5DfkzeDGTN-OPVz8nDz9f76e3X349vt9Ze7yjYcStW6XjEjZIeIDE2vuBK9aRznLdTt4KxCsErIoQFmrOVtr6QVErHnAxeS1efk03HvlOKvA-ai9z5bHEcTMB6yFl3NFJPNDIojaFPMOeGgp-T3Jj1pYHpxrnf6n3O9ONdLcZgHL04XDv0e3fPYSfIMfDwBJs8ShmSC9fmZU8BF14mZ-3zkcPbx6DHpbD0Gi87Prot20b_0y180TaUC</recordid><startdate>20071001</startdate><enddate>20071001</enddate><creator>Broccardo, M.</creator><creator>Guerrini, R.</creator><creator>Morini, G.</creator><creator>Polidori, C.</creator><creator>Agostini, S.</creator><creator>Petrella, C.</creator><creator>Improta, G.</creator><general>Elsevier Inc</general><general>Elsevier Science</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>20071001</creationdate><title>The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions</title><author>Broccardo, M. ; Guerrini, R. ; Morini, G. ; Polidori, C. ; Agostini, S. ; Petrella, C. ; Improta, G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c421t-5db90a678eee0eab9296ba4d225135fdc9e1c967f410acc25b97c67eeb2f26703</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Gastric emptying</topic><topic>Gastric Emptying - drug effects</topic><topic>Opioid Peptides - pharmacology</topic><topic>Rats</topic><topic>Receptors, Opioid - agonists</topic><topic>Secretion and ulcers</topic><topic>Stomach - drug effects</topic><topic>UFP-112</topic><topic>Vertebrates: endocrinology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Broccardo, M.</creatorcontrib><creatorcontrib>Guerrini, R.</creatorcontrib><creatorcontrib>Morini, G.</creatorcontrib><creatorcontrib>Polidori, C.</creatorcontrib><creatorcontrib>Agostini, S.</creatorcontrib><creatorcontrib>Petrella, C.</creatorcontrib><creatorcontrib>Improta, G.</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>Peptides (New York, N.Y. : 1980)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Broccardo, M.</au><au>Guerrini, R.</au><au>Morini, G.</au><au>Polidori, C.</au><au>Agostini, S.</au><au>Petrella, C.</au><au>Improta, G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions</atitle><jtitle>Peptides (New York, N.Y. : 1980)</jtitle><addtitle>Peptides</addtitle><date>2007-10-01</date><risdate>2007</risdate><volume>28</volume><issue>10</issue><spage>1974</spage><epage>1981</epage><pages>1974-1981</pages><issn>0196-9781</issn><eissn>1873-5169</eissn><coden>PPTDD5</coden><abstract>Nociceptin/orphanin FQ (N/OFQ), the endogenous NOP receptor ligand, centrally modulates gastric motor and secretory functions and prevents ethanol-induced gastric lesions in rats. A recently synthesized N/OFQ analog, [(pF)Phe
4Aib
7Arg
14Lys
15]N/OFQ-NH
2 (UFP-112), acts as a highly potent and selective peptide agonist for NOP receptors and produces longer-lasting
in vitro and
in vivo effects in mice than the natural ligand N/OFQ. In this study, we evaluated the effects of centrally (intracerebroventricularly/icv) and peripherally (intraperitoneally/ip) injected UFP-112 on gastric emptying and gastric acid secretion, and on the development of gastric mucosal lesions induced by 50% ethanol in the rat. When injected icv, it dose-dependently delayed gastric emptying of a phenol red meal (by up to 70%), decreased gastric secretion in water-loaded rats after 90 pylorus ligature, and reduced ethanol-induced gastric lesions (by up to 87%). In all three assays, UFP-112 was more effective than N/OFQ. The highly selective NOP receptor antagonist, UFP-101, decreased the efficacy of UFP-112, thus confirming that central NOP receptors mediate inhibitory control on these functional and pathological conditions in rats. Ip injected N/OFQ and UFP-112 induced non-dose-related gastric hypersecretory and antiulcer effects, which UFP-101 partially abolished. Ip N/OFQ appeared equiactive but about 30–100 times less potent than ip UFP-112 in stimulating gastric acid secretion and preventing lesion formation. When ip injected, both UFP-112 and N/OFQ left gastric emptying in rats unchanged, suggesting that peripheral NOP receptors have a role in mediating gastric hypersecretory and antiulcer effects but are not involved in regulating gastric motility. In addition, the inhibitory effects induced by this novel NOP receptor agonist lasted longer than those induced by N/OFQ. In conclusion, UFP-112 is a promising new pharmacological tool for studying the functional roles of the central and peripheral N/OFQ receptor system.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>17765363</pmid><doi>10.1016/j.peptides.2007.07.021</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0196-9781 |
| ispartof | Peptides (New York, N.Y. : 1980), 2007-10, Vol.28 (10), p.1974-1981 |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Animals Biological and medical sciences Fundamental and applied biological sciences. Psychology Gastric emptying Gastric Emptying - drug effects Opioid Peptides - pharmacology Rats Receptors, Opioid - agonists Secretion and ulcers Stomach - drug effects UFP-112 Vertebrates: endocrinology |
| title | The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions |
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