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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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[3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter.

In a continuing effort to identify novel probes with which to study the dopamine transporter (DAT), we discovered that the sigma receptor antagonist, rimcazole, binds with moderate affinity (K(i)=224nM) to the DAT. The results from previous SAR studies suggested that substitution of the carbazole ring system of rimcazole with bis-(4'-fluorophenyl)amine might improve binding affinity and selectivity for the DAT. Thus, a novel series of [3-cis-3,5-dimethyl-(1-piperazinyl)alkyl]bis-(4'-fluorophenyl)amines were synthesized. The most potent compound in this series (9b) displaced [3H]WIN 35,428 binding in rat caudate-putamen (K(i)=17.6nM) with comparable affinity to GBR 12909. Despite high-affinity binding at DAT, and structural similarity to GBR 12909, preliminary studies suggest 9b behaves more like rimcazole than GBR 12909 and does not demonstrate cocaine-like psychostimulant behavior in mice.[1]

References

  1. [3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter. Cao, J., Husbands, S.M., Kopajtic, T., Katz, J.L., Newman, A.H. Bioorg. Med. Chem. Lett. (2001) [Pubmed]
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