Abstract
QSAR models have been used for designing a series of compounds characterized by a N-phenylpiperazinylalkylamino moiety linked to substituted pyridazinones, which have been synthesized. Measurements of the binding affinities of the new compounds toward the alpha(1a)-, alpha(1b)-, and alpha(1d)-AR cloned subtypes as well as the 5-HT(1A) receptor have been done validating, at least in part, the estimations of the theoretical models. This study provides insight into the structure activity relationships of the alpha(1)-ARs ligands and their alpha(1)-AR/5-HT(1A) selectivity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / metabolism
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Animals
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Aorta / drug effects
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Aorta / physiology
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CHO Cells
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Cricetinae
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HeLa Cells
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Humans
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In Vitro Techniques
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Ligands
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Models, Molecular
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Muscle Contraction
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Muscle, Smooth, Vascular / drug effects
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Muscle, Smooth, Vascular / physiology
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / metabolism
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Pyridazines / chemical synthesis*
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Pyridazines / chemistry
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Pyridazines / metabolism
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Quantitative Structure-Activity Relationship
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Radioligand Assay
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Rats
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Rats, Sprague-Dawley
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Receptors, Adrenergic, alpha-1 / metabolism*
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Receptors, Serotonin / metabolism
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Receptors, Serotonin, 5-HT1
Substances
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Adrenergic alpha-Antagonists
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Ligands
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Piperazines
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Pyridazines
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Receptors, Adrenergic, alpha-1
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1