Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.

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Sikazwe DM, Nkansah NT, Altundas R, Zhu XY, Roth BL, Setola V, Ablordeppey SY

Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.

Bioorg Med Chem. 2009 Feb 15;17(4):1716-23. doi: 10.1016/j.bmc.2008.12.054. Epub 2008 Dec 31.

PubMed ID

19155177 [ View in PubMed

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Abstract

Arylcycloalkylamines, such as phenyl piperidines and piperazines and their arylalkyl substituents, constitute pharmacophoric groups exemplified in several antipsychotic agents. A review of previous reports indicates that arylalkyl substituents can improve the potency and selectivity of the binding affinity at D(2)-like receptors. In this paper, we explored the contributions of two key pharmacophoric groups, that is, 4'-fluorobutyrophenones and 3-methyl-7-azaindoles, to the potency and selectivity of synthesized agents at D(2)-like receptors. Preliminary observation of binding affinities indicates that there is little predictability of specific effects of the arylalkyl moieties but the composite structure is responsible for selectivity and potency at these receptors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Haloperidol	Dopamine D2 receptor	Ki (nM)	1.1	N/A	N/A	Details
Haloperidol	Dopamine D3 receptor	Ki (nM)	5.5	N/A	N/A	Details