Matches in DBpedia 2015-10 for { <http://dbpedia.org/resource/JDTic> ?p ?o }
- JDTic abstract "JDTic is a long-acting (irreversible) antagonist of the κ-opioid receptor (KOR). It is selective for the KOR over the μ-opioid receptor (MOR), δ-opioid receptor (DOR), and nociceptin receptor (NOP). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the MOR antagonist alvimopan. In addition, it is structurally distinct from other KOR antagonists such as norbinaltorphimine.JDTic has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to the KOR is not irreversible and its long-acting effects are instead caused by altered activity of c-Jun N-terminal kinases. Animal studies suggest that JDTic may produce antidepressant, anxiolytic, and anti-stress effects, as well as having possible application in the treatment of addiction to cocaine and morphine.The high affinity of JDTic for the KOR suggested that it might be a suitable ligand for promoting the crystallization of this receptor for X-ray crystallographic studies. Such experiments were successful and lead to the publication of the first report of a high-resolution structure of an opioid receptor [ PDB: 4DJH ].JDTic shows robust activity in animal models of depression, anxiety, stress-induced cocaine relapse, and nicotine withdrawal. Upon the initiation of phase I human clinical trials for the treatment of cocaine abuse, however, development was halted due to the incidence of non-sustained ventricular tachycardia, a type of arrhythmia that can potentially be life-threatening. In addition, JDTic showed an unfavorable brain-to-plasma concentration ratio, indicating poor central nervous system penetration. As a result, new KOR antagonists with more favorable drug profiles (e.g., short-acting, improved brain penetration, etc.), such as ALKS-5461 (a combination product of buprenorphine and samidorphan) and CERC-501 (formerly LY-2456302), are being developed in its place.".
- JDTic casNumber "361444-66-8".
- JDTic iupacName "(3R)-7-Hydroxy-N-[(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide".
- JDTic pubchem "9956146".
- JDTic thumbnail JDTic2DCSD2.svg?width=300.
- JDTic wikiPageID "20461967".
- JDTic wikiPageLength "10203".
- JDTic wikiPageOutDegree "49".
- JDTic wikiPageRevisionID "674580997".
- JDTic wikiPageWikiLink 4-Phenylpiperidine.
- JDTic wikiPageWikiLink 4-phenylpiperidine.
- JDTic wikiPageWikiLink 5-Guanidinonaltrindole.
- JDTic wikiPageWikiLink ALKS-5461.
- JDTic wikiPageWikiLink AT-076.
- JDTic wikiPageWikiLink Alvimopan.
- JDTic wikiPageWikiLink Analgesic.
- JDTic wikiPageWikiLink Antagonist_(pharmacology).
- JDTic wikiPageWikiLink Antidepressant.
- JDTic wikiPageWikiLink Anxiety.
- JDTic wikiPageWikiLink Anxiolytic.
- JDTic wikiPageWikiLink Arrhythmia.
- JDTic wikiPageWikiLink BU09059.
- JDTic wikiPageWikiLink Binding_selectivity.
- JDTic wikiPageWikiLink Buprenorphine.
- JDTic wikiPageWikiLink C-Jun_N-terminal_kinases.
- JDTic wikiPageWikiLink CERC-501.
- JDTic wikiPageWikiLink Cardiac_arrhythmia.
- JDTic wikiPageWikiLink Category:Carboxamides.
- JDTic wikiPageWikiLink Category:Irreversible_receptor_antagonists.
- JDTic wikiPageWikiLink Category:Kappa_antagonists.
- JDTic wikiPageWikiLink Category:Opioid_antagonists.
- JDTic wikiPageWikiLink Category:Phenols.
- JDTic wikiPageWikiLink Category:Piperidines.
- JDTic wikiPageWikiLink Category:Synthetic_opioids.
- JDTic wikiPageWikiLink Category:Tetrahydroisoquinolines.
- JDTic wikiPageWikiLink Central_nervous_system.
- JDTic wikiPageWikiLink Clinical_trial.
- JDTic wikiPageWikiLink Cocaine.
- JDTic wikiPageWikiLink Cocaine_dependence.
- JDTic wikiPageWikiLink Delta_opioid_receptor.
- JDTic wikiPageWikiLink Depression_(mood).
- JDTic wikiPageWikiLink Human.
- JDTic wikiPageWikiLink Kappa_opioid_receptor.
- JDTic wikiPageWikiLink Ketobemidone.
- JDTic wikiPageWikiLink Morphine.
- JDTic wikiPageWikiLink Mu_opioid_receptor.
- JDTic wikiPageWikiLink Nicotine_withdrawal.
- JDTic wikiPageWikiLink Nociceptin_receptor.
- JDTic wikiPageWikiLink Norbinaltorphimine.
- JDTic wikiPageWikiLink PF-4455242.
- JDTic wikiPageWikiLink Pethidine.
- JDTic wikiPageWikiLink Phase_I_clinical_trial.
- JDTic wikiPageWikiLink Phases_of_clinical_research.
- JDTic wikiPageWikiLink Receptor_antagonist.
- JDTic wikiPageWikiLink Relapse.
- JDTic wikiPageWikiLink Samidorphan.
- JDTic wikiPageWikiLink Stress_(psychological).
- JDTic wikiPageWikiLink Stress_management.
- JDTic wikiPageWikiLink Substance_dependence.
- JDTic wikiPageWikiLink Ventricular_tachycardia.
- JDTic wikiPageWikiLink Δ-opioid_receptor.
- JDTic wikiPageWikiLink Κ-opioid_receptor.
- JDTic wikiPageWikiLink Μ-opioid_receptor.
- JDTic wikiPageWikiLinkText "JDTic".
- JDTic c "28".
- JDTic casNumber "361444".
- JDTic chemspiderid "8131755".
- JDTic h "39".
- JDTic hasPhotoCollection JDTic.
- JDTic inchi "1".
- JDTic inchikey "ZLVXBBHTMQJRSX-VMGNSXQWBE".
- JDTic iupacName "-7".
- JDTic iupharLigand "7362".
- JDTic molecularWeight "465.626".
- JDTic n "3".
- JDTic o "3".
- JDTic pubchem "9956146".
- JDTic smiles "C[C@H]1CNC[C@H]NC[C@H]3CC4=CC=CO".
- JDTic stdinchi "1".
- JDTic stdinchikey "ZLVXBBHTMQJRSX-VMGNSXQWSA-N".
- JDTic synonyms "JDTic".
- JDTic verifiedfields "changed".
- JDTic verifiedrevid "430261506".
- JDTic watchedfields "changed".
- JDTic width "250".
- JDTic wikiPageUsesTemplate Template:Drugbox.
- JDTic wikiPageUsesTemplate Template:Opioidergics.
- JDTic wikiPageUsesTemplate Template:Reflist.
- JDTic subject Category:Carboxamides.
- JDTic subject Category:Irreversible_receptor_antagonists.
- JDTic subject Category:Kappa_antagonists.
- JDTic subject Category:Opioid_antagonists.
- JDTic subject Category:Phenols.
- JDTic subject Category:Piperidines.
- JDTic subject Category:Synthetic_opioids.
- JDTic subject Category:Tetrahydroisoquinolines.
- JDTic hypernym Antagonist.
- JDTic type Article.
- JDTic type ChemicalSubstance.
- JDTic type Drug.