Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Optically active pyrrolidinylmethylindole analogs related in structure to the benzenesulfonyltryptamine 5-HT(6) receptor antagonist MS-245 were evaluated and their R-isomers were found to bind with affinity higher than their S-enantiomers.
Abate
Carmen
C
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.
Kolanos
Renata
R
Dukat
Malgorzata
M
Setola
Vince
V
Roth
Bryan L
BL
Glennon
Richard A
RA
D001665:Binding Sites; D004347:Drug Interactions; D006801:Humans; D007211:Indoles / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D011985:Receptors, Serotonin / Q000737:chemistry / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000737:chemistry*
D007211:Indoles; C419803:N1-benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine; D011759:Pyrrolidines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines; C097216:serotonin 6 receptor