Abstract
The receptor binding affinities of the three drug candidates 1 (SLV310), 2 (SLV313), and 3 (SLV314) were positioned against the results from nine (a)typical antipsychotic drugs. The receptor binding data from sixteen monoaminergic receptors served as the input in a principal component analysis (PCA). The PCA outcome revealed a unique binding profile of 1, 2, and 3 as compared with the reference compounds 4-8 and 10-12. The weight gain inducing antipsychotics 6-8 clustered in the PCA by scoring strongly negative for factor 1. The hyperprolactinaemia related antipsychotics 4, 5, 10, and 12 clustered by their negative scores for factor 2.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antipsychotic Agents / adverse effects
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Antipsychotic Agents / chemistry*
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Antipsychotic Agents / metabolism
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Basal Ganglia Diseases / chemically induced
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Benzoxazines / adverse effects
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Benzoxazines / chemistry*
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Benzoxazines / metabolism
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Biogenic Monoamines / metabolism
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Humans
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Hyperprolactinemia / chemically induced
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Indoles / adverse effects
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Indoles / chemistry*
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Indoles / metabolism
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Metabolic Diseases / chemically induced
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Phthalimides / adverse effects
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Phthalimides / chemistry*
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Phthalimides / metabolism
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Piperazines / adverse effects
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Piperazines / chemistry*
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Piperazines / metabolism
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Principal Component Analysis
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Pyridines / adverse effects
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Pyridines / chemistry*
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Pyridines / metabolism
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Radioligand Assay
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Receptors, Biogenic Amine / chemistry*
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Receptors, Biogenic Amine / metabolism
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Weight Gain
Substances
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1-(2,3-dihydro-1,4-benzodioxin-5-yl)-4-((5-(4-fluorophenyl)-3-pyridinyl)methyl)piperazine
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2-(4-(4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl)butyl)-phthalimide
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8-(4-(3-(5-fluoro-1H-indol-3-yl)propyl)piperazin-1-yl)-4H-benzo(1,4)oxazin-2-methyl-3-one
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Antipsychotic Agents
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Benzoxazines
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Biogenic Monoamines
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Indoles
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Phthalimides
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Piperazines
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Pyridines
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Receptors, Biogenic Amine