Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists
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چکیده
منابع مشابه
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.
A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties commensurate with an orally available and CNS penetrant profile. The synthesis of a novel bicyclic tetrasubstituted pyridine core template is ou...
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ABSTRACT The neurotransmitter, serotonin (5-hydroxytryptamine, 5-HT), has been linked to such human mental processes as mood sleep and dreaming, sexual behavior, aggression, depression, anxiety, and hallucinogenesis. Serotonin is considered to be relevant in the pathogenesis of several mental and psychosomatic disorders. By understanding the structure of the receptors serotonin binds to, drugs ...
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In vitro, (S)-2-(chloro-5-fluoro-indol-1-yl)-1-methylethylamine 1:1 C4H4O4 and (S)-2-(4,4,7-trimethyl-1,4-dihydro-indeno[1, 2-b]pyrrol-1-yl)-1-methylethylamine 1:1 C4H4O4 exhibited high-affinity binding to the serotonin2C (5HT2C) receptors and stimulated turnover of inositol 1,4,5-triphosphate. Affinity to several of the other 5-HT receptor subtypes and to numerous nonserotonergic receptors was...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2015
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml500507v