Gross, Raymond S. published the artcileDesign and Synthesis of Tricyclic Corticotropin-Releasing Factor-1 Antagonists, Computed Properties of 145349-62-8, the publication is Journal of Medicinal Chemistry (2005), 48(18), 5780-5793, database is CAplus and MEDLINE.
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide should prove to be effective in treating stress and anxiety-related disorders. In an effort to identify antagonists with improved physicochem. properties, new tricyclic CRF1 antagonists were designed, synthesized, and tested for biol. activity. As a result of studies aimed at establishing a relationship between structure and CRF1 binding affinity, NBI 35965 [i.e., (7S)-6-(cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene (I)] was identified as a high-affinity antagonist with a pKi value of 8.5. I proved to be a functional CRF1 antagonist with pIC50 values of 7.1 and 6.9 in the in vitro CRF-stimulated cAMP accumulation and ACTH production assays, resp., and I also reduced CRF or stress induced ACTH production in vivo.
Journal of Medicinal Chemistry published new progress about 145349-62-8. 145349-62-8 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids, name is 2-Chloro-4-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Computed Properties of 145349-62-8.
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