title: Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
abstract: A series of racemic 3-(trans-2-aminomethylcyclopentyl)indoles was synthesized and found to have potent binding to the human serotonin transporter (hSERT). The most active analog was synthesized stereospecifically and the active enantiomer was shown to have high affinity binding to hSERT.
authors: Bristol-Myers SquibbPharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-7660, USA. derek.denhart@bms.com
authors: Derek J
authors: DJ
authors: Denhart
authors: Jeffrey A
authors: JA
authors: Deskus
authors: Jonathan L
authors: JL
authors: Ditta
authors: Qi
authors: Q
authors: Gao
authors: H
authors: H
authors: Dalton King
authors: Edward S
authors: ES
authors: Kozlowski
authors: Zhaoxing
authors: Z
authors: Meng
authors: Melissa A
authors: MA
authors: LaPaglia
authors: Gail K
authors: GK
authors: Mattson
authors: Thaddeus F
authors: TF
authors: Molski
authors: Matthew T
authors: MT
authors: Taber
authors: Nicholas J
authors: NJ
authors: Lodge
authors: Ronald J
authors: RJ
authors: Mattson
authors: John E
authors: JE
authors: Macor
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003517:Cyclopentanes / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008024:Ligands; D008956:Models, Chemical; D011485:Protein Binding; D051381:Rats; D012701:Serotonin / Q000737:chemistry; D017367:Selective Serotonin Reuptake Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000737:chemistry*
chemical_list: D000928:Antidepressive Agents; D003517:Cyclopentanes; D007211:Indoles; D008024:Ligands; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors; D014363:Tryptamines