Abstract
An alpha1a-adrenoceptor-selective antagonist has the potential to be a new benign prostatic hyperplasia drug with reduced side-effects. Modification of the non-selective antagonist BE2254 led to the development of a series of tetralin analogs. Evaluation of these compounds in cloned human alpha1-adrenoceptors resulted in the discovery of an analog that showed selectivity toward the human alpha1a-adrenergic receptor subtype. The compound also showed moderate potency to block human prostate muscle contraction.
MeSH terms
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Adrenergic Antagonists / chemical synthesis*
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Adrenergic Antagonists / chemistry
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Adrenergic Antagonists / pharmacology*
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / pharmacology*
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Drug Design*
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Humans
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Male
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Molecular Structure
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Prostate / drug effects
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Prostate / physiology
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Prostatic Hyperplasia / drug therapy
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Substrate Specificity
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Tetrahydronaphthalenes / chemistry
Substances
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Adrenergic Antagonists
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Adrenergic alpha-Antagonists
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Tetrahydronaphthalenes
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tetralin