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The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists

التفاصيل البيبلوغرافية
العنوان: The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists
المؤلفون: Luis Llamas, William F. Hodnick, Michael J. Robarge, Bayard Huck, Chris Crumrine, Youssef L. Bennani, John J. Harrington, Thomas C. Dent, Alain Stricker-Krongrad, Kurt R. Brunden, Jianping Song
المصدر: Bioorganic & Medicinal Chemistry Letters. 16:2891-2894
بيانات النشر: Elsevier BV, 2006.
سنة النشر: 2006
مصطلحات موضوعية: Agonist, Pyrimidine, medicine.drug_class, media_common.quotation_subject, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Chemical synthesis, Bridged Bicyclo Compounds, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Receptor, Serotonin, 5-HT2C, medicine, Animals, Amines, Receptor, Molecular Biology, media_common, Octane, Aza Compounds, Molecular Structure, Organic Chemistry, Stereoisomerism, Appetite, Small molecule, Rats, 5-HT2C receptor, Pyrimidines, chemistry, Molecular Medicine, Serotonin 5-HT2 Receptor Agonists
الوصف: The 5-HT2C receptor has been implicated in the regulation of appetite. As such, small molecule agonists to this receptor may serve as novel therapies to combat obesity. We describe here the identification, synthesis, and SAR of a 5-HT2C agonist from a unique pyrimidine-diazabicyclo[3.3.0]octane series. This compound displayed good potency at the 5-HT2C receptor, modest selectivity relative to other 5-HT2 receptors, and was efficacious in an acute feeding study in rats.
تدمد: 0960-894X
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61608b27a9e29e14700b2b09f6bb7857
https://doi.org/10.1016/j.bmcl.2006.03.007
حقوق: CLOSED
رقم الأكسشن: edsair.doi.dedup.....61608b27a9e29e14700b2b09f6bb7857
قاعدة البيانات: OpenAIRE
الوصف
تدمد:0960894X