title: 1-Aminoindanes as novel motif with potential atypical antipsychotic properties.
abstract: As part of an on-going effort to investigate the chemical space requirements for D(2)/5-HT(2A) receptor antagonists as atypical antipsychotics, new 1-aminoindanes were synthesized. The replacement of the heterocycle (oxindole) in ziprasidone with a carbocycle (indane) was well tolerated and was found to retain binding affinities for dopamine D(2), serotonin 5-HT(2A), and serotonin 5-HT(1A). Such compounds hold promise as a new chemical motif with atypical antipsychotic properties for the treatment of schizophrenia and related disorders.
authors.affiliation: Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. jamesgraha@gmail.com
authors.forename: James M
authors.initials: JM
authors.lastname: Graham
authors.forename: Linda L
authors.initials: LL
authors.lastname: Coughenour
authors.forename: Bridget M
authors.initials: BM
authors.lastname: Barr
authors.forename: David L
authors.initials: DL
authors.lastname: Rock
authors.forename: Sham S
authors.initials: SS
authors.lastname: Nikam
mesh_terms: D014150:Antipsychotic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000187:drug effects; D006801:Humans; D007189:Indans / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D015394:Molecular Structure; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism
chemical_list: D014150:Antipsychotic Agents; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; D007189:Indans; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2; D044282:Receptor, Serotonin, 5-HT1A; C016992:1-aminoindan