Abstract
Subtype-selective alpha-1a and/or alpha-1d adrenergic receptor antagonists may be useful for the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) with fewer adverse effects than non-selective drugs. A series of 1-arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones has been synthesized, displaying in vitro alpha(1a) and alpha(1d) binding affinity K(i) values in the range of 0.09-38nM with K(i)(alpha1b)/K(i)(alpha1a) and K(i)(alpha1b)/K(i)(alpha1d) selectivity ratios up to 3607-fold.
MeSH terms
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / pharmacology*
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Indicators and Reagents
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Indoles / chemical synthesis*
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Indoles / pharmacology*
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Kinetics
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Ligands
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Magnetic Resonance Spectroscopy
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Piperazines / chemical synthesis*
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Piperazines / pharmacology*
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Radiopharmaceuticals
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Receptors, Adrenergic, alpha-1 / drug effects*
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Stereoisomerism
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Structure-Activity Relationship
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Tetralones
Substances
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Adrenergic alpha-Antagonists
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Indicators and Reagents
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Indoles
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Ligands
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Piperazines
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Radiopharmaceuticals
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Receptors, Adrenergic, alpha-1
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Tetralones
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2-(beta-(3-iodo-4-hydroxyphenyl)ethylaminomethyl)tetralone