Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.

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Linz S, Muller J, Hubner H, Gmeiner P, Troschutz R

Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.

Bioorg Med Chem. 2009 Jul 1;17(13):4448-58. doi: 10.1016/j.bmc.2009.05.015. Epub 2009 May 12.

PubMed ID

19481941 [ View in PubMed

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Abstract

A series of phenylpiperazine-methyl-substituted 1H-pyrrolo[2,3-c]pyridine, imidazo[1,2-c]-, pyrrolo[2,3-d]- and pyrrolo[3,2-d]pyrimidines were prepared as selective dopamine D4-ligands. The pyrrolo[2,3-d]pyrimidine derivatives 12d (K(i)=1,9 nM) and 34 d (K(i)=2,4 nM) as well as the pyrrolo[3,2-d]pyrimidine Mannich base 49f (K(i)=2,8 nM) showed high dopamine D4 receptor activity superior to the atypical antipsychotic agent clozapine.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	28	N/A	N/A	Details
Clozapine	Dopamine D2 receptor	Ki (nM)	41	N/A	N/A	Details
Clozapine	Dopamine D3 receptor	Ki (nM)	960	N/A	N/A	Details