Matches in DBpedia 2016-04 for { <http://wikidata.dbpedia.org/resource/Q18344482> ?p ?o }
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- Q18344482 subject Q15266187.
- Q18344482 subject Q8297683.
- Q18344482 subject Q8390786.
- Q18344482 subject Q8702225.
- Q18344482 subject Q8790228.
- Q18344482 subject Q8808791.
- Q18344482 subject Q8955377.
- Q18344482 subject Q9134654.
- Q18344482 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.".
- Q18344482 atcPrefix "None".
- Q18344482 casNumber "1174130-61-0".
- Q18344482 iupacName "4-(4-{[(2S)-2-(3,5-Dimethylphenyl)-1-pyrrolidinyl]methyl}phenoxy)-3-fluorobenzamide".
- Q18344482 pubchem "44129648".
- Q18344482 thumbnail LY-2456302.svg?width=300.
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- Q18344482 atcPrefix "None".
- Q18344482 casNumber "1174130".
- Q18344482 iupacName "4".
- Q18344482 pubchem "44129648".
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- Q18344482 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.".
- Q18344482 label "CERC-501".
- Q18344482 depiction LY-2456302.svg.