Kulagowski, Janusz J. published the artcile3-[[4-(4-Chlorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine: An Antagonist with High Affinity and Selectivity for the Human Dopamine D4 Receptor, Category: indole-building-block, the main research area is dopamine D4 receptor chlorophenylpiperazinylmethyl pyrrolopyridine.
A topol. similarity search of the Merck sample collection using known dopamine agonists and antagonists as probe structures identified indole I as having modest binding selectivity for cloned human dopamine D4 receptors over D2 and D3 subtypes. Optimization of the amino side chain and introduction of a nitrogen atom into the indole nucleus resulted in L-745,870 (II), having high D4 affinity (Ki 0.43 nM) with 2200 and >5000-fold selectivity over D2 and D3 receptors, resp. Also identified in the course of this work was the piperidinol III which demonstrated the opposite selectivity, being 100-fold binding selective for the D2 receptor.
Journal of Medicinal Chemistry published new progress about Dopamine D4 antagonists. 5654-92-2 belongs to class indole-building-block, name is N,N-Dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-3-yl)methanamine, and the molecular formula is C10H13N3, Category: indole-building-block.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles