1-Aminoindanes as novel motif with potential atypical antipsychotic properties.
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.
Graham
James M
JM
Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. jamesgraha@gmail.com
Coughenour
Linda L
LL
Barr
Bridget M
BM
Rock
David L
DL
Nikam
Sham S
SS
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
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