Clocinnamox inhibits the intravenous self-administration of opioid agonists in rhesus monkeys: comparison with effects on opioid agonist-mediated antinociception
dc.contributor.author | Woods, James H. | en_US |
dc.contributor.author | Zernig, G. | en_US |
dc.contributor.author | Lewis, James W. | en_US |
dc.date.accessioned | 2006-09-08T19:49:06Z | |
dc.date.available | 2006-09-08T19:49:06Z | |
dc.date.issued | 1997-02 | en_US |
dc.identifier.citation | Zernig, G.; Lewis, J. W.; Woods, J. H.; (1997). "Clocinnamox inhibits the intravenous self-administration of opioid agonists in rhesus monkeys: comparison with effects on opioid agonist-mediated antinociception." Psychopharmacology 129(3): 233-242. <http://hdl.handle.net/2027.42/41957> | en_US |
dc.identifier.issn | 0033-3158 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/41957 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=9084061&dopt=citation | en_US |
dc.description.abstract | The effects of CCAM, an insurmountable mu opioid receptor antagonist, were studied on the intravenous self-administration and thermoantinociception of alfentanil and nalbuphine, high- and low-efficacy opioid agonists, respectively, in rhesus monkeys. A single dose of 0.1 mg/kg CCAM IV reduced alfentanil’s reinforcing potency in an FR30 TO 45s schedule 10-fold within a 24-h period. The maximum response rates remained essentially unchanged. At 1 mg/kg, CCAM caused a 300-fold shift of the alfentanil dose-response curve and also depressed the maximum response rates. CCAM also blocked insurmountably responding for nalbuphine, which was essentially abolished in two of three animals after a dose of 0.1 mg/kg CCAM and in all animals after 1 mg/kg. The acute insurmountable antagonism of alfentanil and nalbuphine self-administration by CCAM was used to determine the (relative initial) efficacy values of both agonists. Efficacy values, tau, were 391 for alfentanil and 196 for nalbuphine; the apparent in vivo dissociation constants, K A , were 0.16 mg/kg per injection (i.e., 350 nmol/kg per injection) for alfentanil and 0.14 mg/kg (370 nmol/kg per injection) for nalbuphine. In comparison, in a rhesus monkey 50°C warm-water tail withdrawal assay, the tau values were 11 for alfentanil and 0.92 for nalbuphine, and the K A values were 0.2 mg/kg (440 nmol/kg) for alfentanil and 0.15 mg/kg (400 nmol/kg) for nalbuphine. Therefore, it seems that the higher potency of alfentanil and nalbuphine in self-administration as compared to thermal antinociception in rhesus monkeys is predominantly due to a larger efficacy of the same agonist in self-administration (i.e., a larger receptor pool) rather than differences in apparent in vivo affinity. | en_US |
dc.format.extent | 234166 bytes | |
dc.format.extent | 3115 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Springer-Verlag; Springer-Verlag Berlin Heidelberg | en_US |
dc.subject.other | Legacy | en_US |
dc.subject.other | Clocinnamox | en_US |
dc.subject.other | Receptor Reserve | en_US |
dc.subject.other | Mu Receptors | en_US |
dc.subject.other | Operant Responding | en_US |
dc.subject.other | NIH 10443 | en_US |
dc.subject.other | Antinociception | en_US |
dc.subject.other | Efficacy | en_US |
dc.subject.other | Key Words Apparent in Vivo Affinity | en_US |
dc.subject.other | Opioid Receptors | en_US |
dc.subject.other | Self-administration | en_US |
dc.subject.other | Alfentanil | en_US |
dc.subject.other | Spare Receptors | en_US |
dc.subject.other | Nalbuphine | en_US |
dc.subject.other | Reinforcement | en_US |
dc.title | Clocinnamox inhibits the intravenous self-administration of opioid agonists in rhesus monkeys: comparison with effects on opioid agonist-mediated antinociception | en_US |
dc.type | Article | en_US |
dc.subject.hlbsecondlevel | Psychiatry | en_US |
dc.subject.hlbsecondlevel | Neurosciences | en_US |
dc.subject.hlbsecondlevel | Chemistry | en_US |
dc.subject.hlbsecondlevel | Biological Chemistry | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Department of Pharmacology, University of Michigan, 1301 Medical Science Research Building III, Ann Arbor, MI 48109-0632, USA, US, | en_US |
dc.contributor.affiliationum | Department of Pharmacology, University of Michigan, 1301 Medical Science Research Building III, Ann Arbor, MI 48109-0632, USA, US, | en_US |
dc.contributor.affiliationother | Department of Chemistry, University of Bristol, Bristol, UK, GB, | en_US |
dc.contributor.affiliationumcampus | Ann Arbor | en_US |
dc.identifier.pmid | 9084061 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/41957/1/213-129-3-233_71290233.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1007/s002130050185 | en_US |
dc.identifier.source | Psychopharmacology | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
Files in this item
Remediation of Harmful Language
The University of Michigan Library aims to describe library materials in a way that respects the people and communities who create, use, and are represented in our collections. Report harmful or offensive language in catalog records, finding aids, or elsewhere in our collections anonymously through our metadata feedback form. More information at Remediation of Harmful Language.
Accessibility
If you are unable to use this file in its current format, please select the Contact Us link and we can modify it to make it more accessible to you.