CCB, a novel specific κ opioid agonist, which discriminates between opioid and σ 1 recognition sites

CCB, 6,11 -Dimethyl-1,2,3,4,5,6-hexahydro-3-{[2′-methoxycarbonyl-2′-(4-chlorophenyl) cyclopropyl]methyl}-2,6-methano-3-benzazocin-8-ol, displays specificity and very high affinity for κ opioid receptor types (K 1 = 0.41 ± 0.19 nM). In contrast to other κ opioid agonists, CCB is also selective with r...

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Veröffentlicht in:Life sciences (1973) 1995, Vol.57 (16), p.1487-1495
Hauptverfasser: Ronsisvalle, G., Prezzavento, O., Pasquinucci, L., Marrazzo, A., Vittorio, F., Gomez-Vidal, J.A., Carboni, L., Spampinato, S.
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container_end_page 1495
container_issue 16
container_start_page 1487
container_title Life sciences (1973)
container_volume 57
creator Ronsisvalle, G.
Prezzavento, O.
Pasquinucci, L.
Marrazzo, A.
Vittorio, F.
Gomez-Vidal, J.A.
Carboni, L.
Spampinato, S.
description CCB, 6,11 -Dimethyl-1,2,3,4,5,6-hexahydro-3-{[2′-methoxycarbonyl-2′-(4-chlorophenyl) cyclopropyl]methyl}-2,6-methano-3-benzazocin-8-ol, displays specificity and very high affinity for κ opioid receptor types (K 1 = 0.41 ± 0.19 nM). In contrast to other κ opioid agonists, CCB is also selective with respect to σ 1 sites (K 1 = 1,050 ± 55 nM). CCB displays antinociceptive and sedative effects in the mouse comparable to those of U50,488H and morphine. Naltrexone fully antagonizes these effects. The sedative effects of CCB are blocked in mice pretreated with naltrexone or nor-BNI. CCB and U50,488H produce a superimposable diuresis in rats. Naltrexone and nor-BNI, both are effective in antagonizing the effect. CCB does not produce any stereotyped behavior or ataxia in the behavioral assay in doses up to 40 mg/kg s.c., These findings suggest that CCB might be a useful tool to investigate the physiological role of κ opioid receptors.
doi_str_mv 10.1016/0024-3205(95)02120-8
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In contrast to other κ opioid agonists, CCB is also selective with respect to σ 1 sites (K 1 = 1,050 ± 55 nM). CCB displays antinociceptive and sedative effects in the mouse comparable to those of U50,488H and morphine. Naltrexone fully antagonizes these effects. The sedative effects of CCB are blocked in mice pretreated with naltrexone or nor-BNI. CCB and U50,488H produce a superimposable diuresis in rats. Naltrexone and nor-BNI, both are effective in antagonizing the effect. CCB does not produce any stereotyped behavior or ataxia in the behavioral assay in doses up to 40 mg/kg s.c., These findings suggest that CCB might be a useful tool to investigate the physiological role of κ opioid receptors.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/0024-3205(95)02120-8</identifier><identifier>PMID: 7564893</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer ; Analgesics - pharmacology ; Animals ; Benzomorphans - pharmacology ; Binding, Competitive ; CCB ; Male ; Mice ; Morphine - pharmacology ; Naltrexone - pharmacology ; Pyrrolidines - pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptors, Opioid, delta - drug effects ; Receptors, Opioid, kappa - agonists ; Receptors, Opioid, kappa - drug effects ; specific κ opioid agonist ; δ binding ; κ binding ; μ binding ; σ 1 binding</subject><ispartof>Life sciences (1973), 1995, Vol.57 (16), p.1487-1495</ispartof><rights>1995</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0024-3205(95)02120-8$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,4024,27923,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7564893$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ronsisvalle, G.</creatorcontrib><creatorcontrib>Prezzavento, O.</creatorcontrib><creatorcontrib>Pasquinucci, L.</creatorcontrib><creatorcontrib>Marrazzo, A.</creatorcontrib><creatorcontrib>Vittorio, F.</creatorcontrib><creatorcontrib>Gomez-Vidal, J.A.</creatorcontrib><creatorcontrib>Carboni, L.</creatorcontrib><creatorcontrib>Spampinato, S.</creatorcontrib><title>CCB, a novel specific κ opioid agonist, which discriminates between opioid and σ 1 recognition sites</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>CCB, 6,11 -Dimethyl-1,2,3,4,5,6-hexahydro-3-{[2′-methoxycarbonyl-2′-(4-chlorophenyl) cyclopropyl]methyl}-2,6-methano-3-benzazocin-8-ol, displays specificity and very high affinity for κ opioid receptor types (K 1 = 0.41 ± 0.19 nM). In contrast to other κ opioid agonists, CCB is also selective with respect to σ 1 sites (K 1 = 1,050 ± 55 nM). CCB displays antinociceptive and sedative effects in the mouse comparable to those of U50,488H and morphine. Naltrexone fully antagonizes these effects. The sedative effects of CCB are blocked in mice pretreated with naltrexone or nor-BNI. CCB and U50,488H produce a superimposable diuresis in rats. Naltrexone and nor-BNI, both are effective in antagonizing the effect. 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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
Analgesics - pharmacology
Animals
Benzomorphans - pharmacology
Binding, Competitive
CCB
Male
Mice
Morphine - pharmacology
Naltrexone - pharmacology
Pyrrolidines - pharmacology
Rats
Rats, Sprague-Dawley
Receptors, Opioid, delta - drug effects
Receptors, Opioid, kappa - agonists
Receptors, Opioid, kappa - drug effects
specific κ opioid agonist
δ binding
κ binding
μ binding
σ 1 binding
title CCB, a novel specific κ opioid agonist, which discriminates between opioid and σ 1 recognition sites
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