Author/Authors :
Yuching Tsai، نويسنده , , Malgorzata Dukat، نويسنده , , Abdelmalik Slassi*، نويسنده , , Neil MacLean، نويسنده , , Lidia Demchyshyn، نويسنده , , Jason E. Savage، نويسنده , , Bryan L. Roth، نويسنده , , Sandy Hufesein، نويسنده , , Mase Lee، نويسنده , , Richard A. Glennon، نويسنده ,
Abstract :
N1-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (BS/5-OMe DMT; 5) was shown to bind at human 5-HT6 serotonin receptors with high affinity (Ki=2.3 nM) relative to serotonin (Ki=78 nM). Structural variation failed to result in significantly enhanced affinity. BS/5-OMe DMT acts as an antagonist of 5-HT-stimulated adenylate cyclase (pA2=8.88 nM) and may represent the first member of a novel class of 5-HT6 antagonists.
