New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands.
A series of compounds in which various halogen substituents were incorporated into a phenyl ring of a tris-(phenylalkyl)amine scaffold, was synthesized and evaluated for affinity to h5-HT2 receptors. In general, all compounds were found to have good affinity for the 5-HT2B receptor and were selective over 5-HT2A and 5-HT2C receptors. Compound 9i was the most selective compound in this study and is the highest affinity 5-HT2B receptor ligand bearing a tris-(phenylalkyl)amine scaffold to date.
Chemistry Dept., Hunter College, City University Of New York, 695 Park Ave, New York, NY 10065, USA; CUNY Graduate Center, 365 5th Avenue, New York, NY 10016, USA.
Nirav
N
Kapadia
Chemistry Dept., Hunter College, City University Of New York, 695 Park Ave, New York, NY 10065, USA.
Shahrear
S
Ahmed
Chemistry Dept., Hunter College, City University Of New York, 695 Park Ave, New York, NY 10065, USA; CUNY Graduate Center, 365 5th Avenue, New York, NY 10016, USA.
Wayne W
WW
Harding
D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism*; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism; D013329:Structure-Activity Relationship
D000588:Amines; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D044403:Receptor, Serotonin, 5-HT2B; D044405:Receptor, Serotonin, 5-HT2C
5-HT(2A); 5-HT(2B); CNS; Tris-(phenylalkyl)amine