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Dibenzazecines are a novel class of dopamine receptor antagonists, characterized by their high affinities as well as their tendency for D1 selectivity. Hitherto, the most active dibenzazecines were phenolic in nature; a 3‐OH substituent was found to result in the highest affinities. However, the phenolic nature of these compounds mostly renders them unsuitable for in vivo application, due to the poor...
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...
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