Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 오세관 | * |
dc.contributor.author | 정재철 | * |
dc.date.accessioned | 2016-08-28T10:08:26Z | - |
dc.date.available | 2016-08-28T10:08:26Z | - |
dc.date.issued | 2013 | * |
dc.identifier.issn | 1747-0277 | * |
dc.identifier.other | OAK-9755 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/223427 | - |
dc.description.abstract | A series of 3,4,5-trimethoxycinnamic acid derivatives was prepared and evaluated for antinarcotic effects on morphine dependence in mice and binding affinities on serotonergic receptors. The key synthetic strategies involve generation of ketones 6-7, esters 9-12 through condensation reaction, and amides 13-19 via coupling reaction using 1-hydroxybenzotriazole/ethyl(dimethylaminopropryl)carbodiimide system in high yield. We found that the naloxone-induced morphine withdrawal syndrome was significantly suppressed by new synthetic 3,4,5-trimethoxycinnamic acid derivatives (20mg/kg/day). Most of 3,4,5-trimethoxycinnamic acid derivatives were found to have high affinity to 5-HT1A receptor. The naloxone-induced morphine withdrawal syndrome was attenuated by (+)8-OH-DPAT (0.1mg/kg/day, i.p.), a 5-HT1A receptor agonist. In cortical neuronal cells, (+)8-OH-DPAT (1μm) produced an elevation of the pERK 1/2 expression, and the elevated pERK levels were inhibited by WAY 100635, a 5-HT1A receptor-specific antagonist. Interestingly, the pERK levels were increased by the 3,4,5-trimethoxycinnamic acid derivatives and the derivatives-mediated changes in pERK levels were blocked by the WAY 100635. These results suggested that new synthetic 3,4,5-trimethoxycinnamic acid derivatives have a potential antinarcotic effect through acting as a 5-HT1A receptor agonist in mice. © 2012 John Wiley & Sons A/S. | * |
dc.language | English | * |
dc.title | Synthesis and Evaluation of a Series of 3,4,5-Trimethoxycinnamic Acid Derivatives as Potential Antinarcotic Agents | * |
dc.type | Article | * |
dc.relation.issue | 3 | * |
dc.relation.volume | 81 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 389 | * |
dc.relation.lastpage | 398 | * |
dc.relation.journaltitle | Chemical Biology and Drug Design | * |
dc.identifier.doi | 10.1111/cbdd.12087 | * |
dc.identifier.wosid | WOS:000314985900008 | * |
dc.identifier.scopusid | 2-s2.0-84873747639 | * |
dc.author.google | Jung J.-C. | * |
dc.author.google | Moon S. | * |
dc.author.google | Min D. | * |
dc.author.google | Park W.K. | * |
dc.author.google | Jung M. | * |
dc.author.google | Oh S. | * |
dc.contributor.scopusid | 오세관(7404103757) | * |
dc.contributor.scopusid | 정재철(7402897187) | * |
dc.date.modifydate | 20240123112233 | * |