Binding of beta-carbolines at 5-HT(2) serotonin receptors.
A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-beta-carbolines was examined at 5-HT(2A) and 5-HT(2C) serotonin receptors. Whereas most of the methoxy-substituted derivatives typically displayed affinities similar to their unsubstituted parents, certain (particularly 8-substituted) bromo derivatives displayed enhanced affinity. A binding profile was obtained for selected beta-carbolines.
Grella
Brian
B
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.
Teitler
Milt
M
Smith
Carol
C
Herrick-Davis
Katharine
K
Glennon
R A
RA
D001665:Binding Sites; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D011485:Protein Binding; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism; D044348:Receptors, Serotonin, 5-HT2 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D002243:Carbolines; D044402:Receptor, Serotonin, 5-HT2A; D044403:Receptor, Serotonin, 5-HT2B; D044405:Receptor, Serotonin, 5-HT2C; D044348:Receptors, Serotonin, 5-HT2