PMID- 17379253 OWN - NLM STAT- MEDLINE DCOM- 20070612 LR - 20161122 IS - 0024-3205 (Print) IS - 0024-3205 (Linking) VI - 80 IP - 19 DP - 2007 Apr 17 TI - Antagonism of phosphoramidon-induced antinociception in mice by mu- but not kappa-opioid receptor blockers. PG - 1816-20 AB - Intracerebroventricular (i.c.v.) administration of the neutral endopeptidase 24.11-inhibitor phosphoramidon evoked a dose-dependent antinociceptive effect in the mouse acetic acid abdominal constriction test. The present study was conducted to identify the opioid receptor subtype(s) that mediate phosphoramidon antinociception in this paradigm. Mice were pretreated with different opioid antagonists prior to being challenged with phosphoramidon, i.c.v., the mu-opioid agonist sufentanil, s.c., or the kappa-opioid agonist U-50,488H, s.c. Naltrexone significantly attenuated phosphoramidon-induced antinociception at an i.c.v. dose that also blocked both sufentanil and U-50,488H. The mu-opioid antagonist beta-funaltrexamine (beta-FNA) blocked phosphoramidon and sufentanil at an i.c.v. dose that did not block U-50,488H. The kappa-opioid antagonist nor-binaltorphimine (nor-BNI) produced dose-related effects. A low dose (10 microg) of nor-BNI had no effect on either phosphoramidon or sufentanil but did reduce U-50,488H antinociception. A higher dose (30 microg) of nor-BNI blocked phosphoramidon, sufentanil, and U-50,488H, suggesting a loss of kappa-opioid receptor selectivity at this dose. These findings suggest that mu- but not kappa-opioid receptors mediate phosphoramidon-induced antinociception in the abdominal constriction test. FAU - Pruhs, Ronald J AU - Pruhs RJ AD - Department of Pediatric Dentistry, Marquette University School of Dentistry, Milwaukee, WI 53201-1881, United States. FAU - Pena, Roehl T AU - Pena RT FAU - Quock, Raymond M AU - Quock RM LA - eng GR - R01 DE006894-06/DE/NIDCR NIH HHS/United States GR - DE-10047/DE/NIDCR NIH HHS/United States GR - DE-06894/DE/NIDCR NIH HHS/United States GR - R01 DA010343-03/DA/NIDA NIH HHS/United States GR - R01 DA010047-04/DA/NIDA NIH HHS/United States PT - Journal Article PT - Research Support, N.I.H., Extramural DEP - 20070222 PL - Netherlands TA - Life Sci JT - Life sciences JID - 0375521 RN - 0 (Glycopeptides) RN - 0 (Narcotic Antagonists) RN - 0 (Receptors, Opioid, kappa) RN - 0 (Receptors, Opioid, mu) RN - 5S6W795CQM (Naltrexone) RN - 67198-13-4 (3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer) RN - 72782-05-9 (beta-funaltrexamine) RN - T3G94E2LB1 (phosphoramidon) SB - IM MH - 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer/pharmacology MH - *Analgesia MH - Animals MH - Glycopeptides/antagonists & inhibitors/*pharmacology MH - Male MH - Mice MH - Mice, Inbred ICR MH - Naltrexone/analogs & derivatives/pharmacology MH - Narcotic Antagonists/pharmacology MH - Receptors, Opioid, kappa/agonists/antagonists & inhibitors/physiology MH - Receptors, Opioid, mu/agonists/antagonists & inhibitors/*physiology EDAT- 2007/03/24 09:00 MHDA- 2007/06/15 09:00 CRDT- 2007/03/24 09:00 PHST- 2006/09/06 00:00 [received] PHST- 2007/01/27 00:00 [revised] PHST- 2007/02/15 00:00 [accepted] PHST- 2007/03/24 09:00 [pubmed] PHST- 2007/06/15 09:00 [medline] PHST- 2007/03/24 09:00 [entrez] AID - S0024-3205(07)00178-6 [pii] AID - 10.1016/j.lfs.2007.02.019 [doi] PST - ppublish SO - Life Sci. 2007 Apr 17;80(19):1816-20. doi: 10.1016/j.lfs.2007.02.019. Epub 2007 Feb 22.