dc.contributor.author | Sun, Jian-feng | en_US |
dc.contributor.author | Wang, Yu-hua | en_US |
dc.contributor.author | Li, Fu-ying | en_US |
dc.contributor.author | Lu, Gang | en_US |
dc.contributor.author | Tao, Yi-min | en_US |
dc.contributor.author | Cheng, Yun | en_US |
dc.contributor.author | Chen, Jie | en_US |
dc.contributor.author | Xu, Xue-jun | en_US |
dc.contributor.author | Chi, Zhi-qiang | en_US |
dc.contributor.author | Neumeyer, John L | en_US |
dc.contributor.author | Zhang, Ao | en_US |
dc.contributor.author | Liu, Jing-gen | en_US |
dc.date.accessioned | 2014-10-01T14:29:11Z | |
dc.date.issued | 2010 | en_US |
dc.identifier.citation | Sun, J., Y. Wang, F. Li, G. Lu, Y. Tao, Y. Cheng, J. Chen, et al. 2010. “Effects of ATPM-ET, a novel κ agonist with partial μ activity, on physical dependence and behavior sensitization in mice.” Acta Pharmacologica Sinica 31 (12): 1547-1552. doi:10.1038/aps.2010.164. http://dx.doi.org/10.1038/aps.2010.164. | en |
dc.identifier.issn | 1671-4083 | en |
dc.identifier.uri | http://nrs.harvard.edu/urn-3:HUL.InstRepos:12987362 | |
dc.description.abstract | Aim: To investigate the effects of ATPM-ET [(−)-3-N-Ethylaminothiazolo [5,4-b]-N-cyclopropylmethylmorphinan hydrochloride] on physical dependence and behavioral sensitization to morphine in mice. Methods: The pharmacological profile of ATPM-ET was characterized using competitive binding and GTPγS binding assays. We then examined the antinociceptive effects of ATPM-ET in the hot plate test. Morphine dependence assay and behavioral sensitization assay were used to determine the effect of ATPM-ET on physical dependence and behavior sensitization to morphine in mice. Results: The binding assay indicated that ATPM-ET ATPM-ET exhibited a high affinity to both κ- and μ-opioid receptors with Ki values of 0.15 nmol/L and 4.7 nmol/L, respectively, indicating it was a full κ-opioid receptor agonist and a partial μ-opioid receptor agonist. In the hot plate test, ATPM-ET produced a dose-dependent antinociceptive effect, with an ED50 value of 2.68 (2.34–3.07) mg/kg. Administration of ATPM-ET (1 and 2 mg/kg, sc) prior to naloxone (3.0 mg/kg, sc) injection significantly inhibited withdrawal jumping of mice. In addition, ATPM-ET (1 and 2 mg/kg, sc) also showed a trend toward decreasing morphine withdrawal-induced weight loss. ATPM-ET (1.5 and 3 mg/kg, sc) 15 min before the morphine challenge significantly inhibited the morphine-induced behavior sensitization (P<0.05). Conclusion: ATPM-ET may have potential as a therapeutic agent for the treatment of drug abuse. | en |
dc.language.iso | en_US | en |
dc.publisher | Nature Publishing Group | en |
dc.relation.isversionof | doi:10.1038/aps.2010.164 | en |
dc.relation.hasversion | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4002947/pdf/ | en |
dash.license | LAA | en_US |
dc.subject | behavioral sensitization | en |
dc.subject | mu opioid receptors | en |
dc.subject | morphine | en |
dc.subject | kappa opioid receptors | en |
dc.subject | physical dependence | en |
dc.subject | addiction | en |
dc.title | Effects of ATPM-ET, a novel κ agonist with partial μ activity, on physical dependence and behavior sensitization in mice | en |
dc.type | Journal Article | en_US |
dc.description.version | Version of Record | en |
dc.relation.journal | Acta Pharmacologica Sinica | en |
dash.depositing.author | Neumeyer, John L | en_US |
dc.date.available | 2014-10-01T14:29:11Z | |
dc.identifier.doi | 10.1038/aps.2010.164 | * |
dash.authorsordered | false | |
dash.contributor.affiliated | Neumeyer, John | |