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1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT6 serotonin receptor ligands

✍ Scribed by Chul Min Park; Jin Il Choi; Jung Hwan Choi; So Young Kim; Woo Kyu Park; Churl Min Seong


Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
536 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis


a b s t r a c t Piperazinyl derivatives of 1-(arylsulfonyl)-2,3-dihydro-1H-quinolin-4-ones have been identified with high binding affinities for 5-HT 6 receptor. In particular, 2-methyl-5-(N-methyl-piperazin-1-yl)-1-(naphthalene-2-sulfonyl)-2,3-dihydro-1H-quinolin-4-one (8g) exhibits high binding affinity toward 5-HT 6 (IC 50 = 8 nM) receptor with good selectivity over other serotonin and dopamine receptors.


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