1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.
Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT(6) receptor ligands, among which N,N-dimethyl-N-(2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl)amine 8t and N-methyl-N-(2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl)amine 8u showed high affinity for 5-HT(6) receptors with K(i)=3.7 and 5.7 nM, respectively.
Bernotas
Ronald
R
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. bernotr@wyeth.com
Lenicek
Steven
S
Antane
Schuyler
S
Zhang
Guo Ming
GM
Smith
Deborah
D
Coupet
Joseph
J
Harrison
Boyd
B
Schechter
Lee E
LE
D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology; D001667:Binding, Competitive; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship
D000588:Amines; D007211:Indoles; D008024:Ligands; D011985:Receptors, Serotonin; C097216:serotonin 6 receptor