Abstract
The significant contribution of folded conformation (2) of the anxiolytic tandospirone (1) in aqueous solution was verified by dynamic 1H NMR. A structurally rigid mimic of 2 was designed and synthesized to evaluate the implication of 2 towards neuroleptic receptor binding. The designed structures provided a new rigid scaffold for dopamine D4 ligands.
MeSH terms
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Drug Design
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Indicators and Reagents
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Isoindoles
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Kinetics
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Ligands
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Conformation
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Molecular Mimicry
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Piperazines / chemistry*
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Pyrimidines / chemistry*
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Receptors, Dopamine D2 / drug effects*
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Receptors, Dopamine D4
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Receptors, Serotonin / drug effects
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists / chemistry*
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Solutions
Substances
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Indicators and Reagents
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Isoindoles
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Ligands
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Piperazines
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Pyrimidines
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Receptors, Dopamine D2
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists
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Solutions
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Receptors, Dopamine D4
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tandospirone