1-Aminoindanes as novel motif with potential atypical antipsychotic properties.

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Graham JM, Coughenour LL, Barr BM, Rock DL, Nikam SS

1-Aminoindanes as novel motif with potential atypical antipsychotic properties.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):489-93. Epub 2007 Dec 3.

PubMed ID

18160289 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Ziprasidone	5-hydroxytryptamine receptor 1A	Ki (nM)	4	N/A	N/A	Details
Ziprasidone	5-hydroxytryptamine receptor 2A	Ki (nM)	0.08	N/A	N/A	Details
Ziprasidone	Dopamine D2 receptor	Ki (nM)	5	N/A	N/A	Details