204650-33-9Relevant academic research and scientific papers
Serotonin receptor binding benzo[e]isoindoles and benzo[h]isoquinolines
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, (2008/06/13)
Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
Syntheses of O-Methylasparvenone-derived Serotonin-receptor Antagonists
Boes, Michael,Stadler, Heinz,Wichmann, Juergen,Jenck, Francois,Martin, James R.,et al.
, p. 525 - 538 (2007/10/03)
Based on O-methylasparvenone (1), a N-free 5HT2C antagonist with moderate affinity (pKi = 6.7), derivatives bearing dimethylamino (7), (dimethylamino)methyl (17, 18, 21, and 22), and aminomethyl substituents (26) in place of the benzylic OH group of 1 as well as pyrrolidine- (33) and piperidine-fused derivatives (29, 43, and 45) were synthesized.In contrast to the lead structure 1, these new ligands were active in vivo in the rat.The tricycles 33 and 45 display high affinities for the 5HT2C receptor (pKi = 8).
