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Synonyms: MK 0249 | MK0249
Compound class: Synthetic organic
Comment: H3 receptor inverse agonists may be efficacious for central nervous system disorders, including excessive daytime sleepiness, attention deficit hyperactivity disorder, Alzheimer disease, ethanol addiction, and obesity .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Egan M, Yaari R, Liu L, Ryan M, Peng Y, Lines C, Michelson D. (2012)
Pilot randomized controlled study of a histamine receptor inverse agonist in the symptomatic treatment of AD.
Curr Alzheimer Res, 9 (4): 481-90. [PMID:22272611]
2. Nagase T, Mizutani T, Ishikawa S, Sekino E, Sasaki T, Fujimura T, Ito S, Mitobe Y, Miyamoto Y, Yoshimoto R et al.. (2008)
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
J Med Chem, 51 (15): 4780-9. [PMID:18598020]
3. Panula P, Chazot PL, Cowart M, Gutzmer R, Leurs R, Liu WL, Stark H, Thurmond RL, Haas HL. (2015)
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Pharmacol Rev, 67 (3): 601-55. [PMID:26084539]
4. Van Laere KJ, Sanabria-Bohórquez SM, Mozley DP, Burns DH, Hamill TG, Van Hecken A, De Lepeleire I, Koole M, Bormans G, de Hoon J et al.. (2014)
(11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists.
J Nucl Med, 55 (1): 65-72. [PMID:24263088]