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To further investigate SAR in the class of azecine‐type dopamine receptor antagonists, we synthesized a series of derivatives, substituted at the indole‐NH of the lead compound LE300 by different alkyl chains in addition to phenylpropyl, allyl, propargyl, and acetyl residues. The affinities of the target compounds for all human dopamine receptors (D1–D5) were investigated by radioligand binding assay...
The affinities of tetrahydroprotoberberines for dopamine receptors dramatically decrease after cleaving the central C‐N bond to the analogous ten‐membered dibenzo[c,g]azecines [1]. In the present work, we also synthesized eleven‐membered homologues of these heterocycles and measured the affinities of the resulting dibenzazaundecenes and their underlying homoberberines for human dopamine receptors...
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