Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors.
Despite possessing a common tryptaminergic scaffold, examination of 28 (i.e., 14 pairs of) compounds suggests that N1-unsubstituted and N1-benzenesulfonyltryptamines likely bind at h5-HT6 receptors in a dissimilar manner (r2=0.201). Additionally, an examination of two rotationally constrained N1-benzenesulfonyltryptamine analogs indicates that a non-coplanar relationship between the two aryl groups might be preferred for interaction with the receptors.
Kolanos
Renata
R
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.
Dukat
Małgorzata
M
Roth
Bryan L
BL
Glennon
Richard A
RA
D004347:Drug Interactions; D006801:Humans; D011485:Protein Binding; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000737:chemistry / Q000494:pharmacology*
C419803:N1-benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines; C097216:serotonin 6 receptor