Matches in DBpedia 2016-04 for { <http://dbpedia.org/resource/CERC-501> ?p ?o }
- CERC-501 abstract "CERC-501 (originally known as LY-2456302) is a potent, selective, short-acting (non-\"inactivating\") antagonist of the κ-opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively; ~30-fold selectivity for the KOR) that was originally developed by Eli Lilly. In February 2015, Cerecor Inc. announced that they had acquired the rights from Eli Lilly to develop and commercialize LY-2456302 (under the new developmental code name of CERC-501).CERC-501 is under development for the treatment of major depressive disorder and substance use disorders including alcoholism, nicotine addiction, and illicit drug dependence. As of 2016, it has reached phase II clinical trials as an augmentation to antidepressant therapy for treatment-resistant depression. In animal models of depression, CERC-501 has been found to have potent synergistic efficacy in combination with other antidepressants such as citalopram and imipramine. A phase II study of CERC-501 in heavy smokers will be commenced in early 2016 and results of the study are expected before the end of 2016.In December 2015, the results of a human pharmacokinetic study of CERC-501 were released. CERC-501 was shown to reproducibly penetrate the blood-brain-barrier, and positron emission tomography imaging revealed that brain KORs were almost completely saturated by the drug 2.5 hours following a single dose of 10 mg, which supported the 4 mg to 25 mg dosages that CERC-501 is being explored at in clinical trials. Occupancy was 35% for a 0.5 mg dose and 94% for a 10 mg dose. At 24 hours post-dose, receptor occupancy was 19% for 0.5 mg and 82% for 25 mg. No serious side effects were observed, and all side effects seen were mild to moderate and not considered to be due to CERC-501.CERC-501 has been found to dose-dependently block fentanyl-induced miosis at 25 mg and 60 mg in humans (with minimal to no blockade at doses of 4 to 10 mg), indicating that the drug significantly occupies and antagonizes the MOR at a dose of at least 25 mg but not of 10 mg or less.".
- CERC-501 atcPrefix "None".
- CERC-501 casNumber "1174130-61-0".
- CERC-501 iupacName "4-(4-{[(2S)-2-(3,5-Dimethylphenyl)-1-pyrrolidinyl]methyl}phenoxy)-3-fluorobenzamide".
- CERC-501 pubchem "44129648".
- CERC-501 thumbnail LY-2456302.svg?width=300.
- CERC-501 wikiPageExternalLink 800032395.
- CERC-501 wikiPageExternalLink cerc-501.php.
- CERC-501 wikiPageID "43221610".
- CERC-501 wikiPageLength "9109".
- CERC-501 wikiPageOutDegree "42".
- CERC-501 wikiPageRevisionID "701855734".
- CERC-501 wikiPageWikiLink Adjuvant_therapy.
- CERC-501 wikiPageWikiLink Alcoholism.
- CERC-501 wikiPageWikiLink Antidepressant.
- CERC-501 wikiPageWikiLink BU09059.
- CERC-501 wikiPageWikiLink Blood–brain_barrier.
- CERC-501 wikiPageWikiLink samidorphan.
- CERC-501 wikiPageWikiLink Category:Antidepressants.
- CERC-501 wikiPageWikiLink Category:Benzamides.
- CERC-501 wikiPageWikiLink Category:Drug_rehabilitation.
- CERC-501 wikiPageWikiLink Category:Fluoroarenes.
- CERC-501 wikiPageWikiLink Category:Kappa_antagonists.
- CERC-501 wikiPageWikiLink Category:Opioid_antagonists.
- CERC-501 wikiPageWikiLink Category:Pyrrolidines.
- CERC-501 wikiPageWikiLink Category:Synthetic_opioids.
- CERC-501 wikiPageWikiLink Cerecor.
- CERC-501 wikiPageWikiLink Chain_smoking.
- CERC-501 wikiPageWikiLink Citalopram.
- CERC-501 wikiPageWikiLink Clinical_trial.
- CERC-501 wikiPageWikiLink Depression_(mood).
- CERC-501 wikiPageWikiLink Eli_Lilly.
- CERC-501 wikiPageWikiLink Fentanyl.
- CERC-501 wikiPageWikiLink Illegal_drug_trade.
- CERC-501 wikiPageWikiLink Imipramine.
- CERC-501 wikiPageWikiLink JDTic.
- CERC-501 wikiPageWikiLink LY-2459989.
- CERC-501 wikiPageWikiLink Major_depressive_disorder.
- CERC-501 wikiPageWikiLink Miosis.
- CERC-501 wikiPageWikiLink Model_organism.
- CERC-501 wikiPageWikiLink Nicotine.
- CERC-501 wikiPageWikiLink Oral_administration.
- CERC-501 wikiPageWikiLink PF-4455242.
- CERC-501 wikiPageWikiLink Pharmacokinetics.
- CERC-501 wikiPageWikiLink Phases_of_clinical_research.
- CERC-501 wikiPageWikiLink Positron_emission_tomography.
- CERC-501 wikiPageWikiLink Receptor_antagonist.
- CERC-501 wikiPageWikiLink Side_effect.
- CERC-501 wikiPageWikiLink Substance_dependence.
- CERC-501 wikiPageWikiLink Substance_use_disorder.
- CERC-501 wikiPageWikiLink Treatment-resistant_depression.
- CERC-501 wikiPageWikiLink Δ-opioid_receptor.
- CERC-501 wikiPageWikiLink Κ-opioid_receptor.
- CERC-501 wikiPageWikiLink Μ-opioid_receptor.
- CERC-501 wikiPageWikiLinkText "CERC-501".
- CERC-501 atcPrefix "None".
- CERC-501 c "26".
- CERC-501 casNumber "1174130".
- CERC-501 chemspiderid "28424203".
- CERC-501 eliminationHalfLife "-144000.0".
- CERC-501 f "1".
- CERC-501 h "27".
- CERC-501 inchi "1".
- CERC-501 inchikey "ZHPMYDSXGRRERG-DEOSSOPVBF".
- CERC-501 iupacName "4".
- CERC-501 molecularWeight "418.503".
- CERC-501 n "2".
- CERC-501 o "2".
- CERC-501 pubchem "44129648".
- CERC-501 routesOfAdministration Oral_administration.
- CERC-501 smiles "CC1=CCC".
- CERC-501 stdinchi "1".
- CERC-501 stdinchikey "ZHPMYDSXGRRERG-DEOSSOPVSA-N".
- CERC-501 wikiPageUsesTemplate Template:Antiaddictives.
- CERC-501 wikiPageUsesTemplate Template:Antidepressants.
- CERC-501 wikiPageUsesTemplate Template:Drugbox.
- CERC-501 wikiPageUsesTemplate Template:Nervous-system-drug-stub.
- CERC-501 wikiPageUsesTemplate Template:Opioidergics.
- CERC-501 wikiPageUsesTemplate Template:Reflist.
- CERC-501 subject Category:Antidepressants.
- CERC-501 subject Category:Benzamides.
- CERC-501 subject Category:Drug_rehabilitation.
- CERC-501 subject Category:Fluoroarenes.
- CERC-501 subject Category:Kappa_antagonists.
- CERC-501 subject Category:Opioid_antagonists.
- CERC-501 subject Category:Pyrrolidines.
- CERC-501 subject Category:Synthetic_opioids.
- CERC-501 hypernym Antagonist.
- CERC-501 type ChemicalSubstance.
- CERC-501 type Drug.
- CERC-501 type ChemicalObject.
- CERC-501 type Thing.
- CERC-501 type Q8386.
- CERC-501 comment "CERC-501 (originally known as LY-2456302) is a potent, selective, short-acting (non-\"inactivating\") antagonist of the κ-opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively; ~30-fold selectivity for the KOR) that was originally developed by Eli Lilly. In February 2015, Cerecor Inc.".
- CERC-501 label "CERC-501".
- CERC-501 sameAs Q18344482.
- CERC-501 sameAs m.0114mr1q.
- CERC-501 sameAs Q18344482.
- CERC-501 wasDerivedFrom CERC-501?oldid=701855734.
- CERC-501 depiction LY-2456302.svg.