Abstract
Benign prostatic hyperplasia can be managed pharmacologically with alpha-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the alpha-1a receptor subtype may offer advantages in clinical applications with respect to hypotensive side effects. The N-alkylated saccharins reported here represent a new class of subtype selective alpha-1a adrenergic receptor antagonists which demonstrate potent effects on prostate function in vivo and are devoid of blood pressure side effects.
MeSH terms
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Adrenergic alpha-1 Receptor Antagonists*
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / pharmacology
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Alkylation
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Animals
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Aorta / drug effects
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CHO Cells
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Cell Line
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Cricetinae
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Dogs
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Drug Design*
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Finasteride / chemistry
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Finasteride / pharmacology
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Humans
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In Vitro Techniques
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Male
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Models, Chemical
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Prazosin / analogs & derivatives
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Prazosin / chemistry
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Prazosin / pharmacology
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Prostate / drug effects
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Rats
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Receptors, Adrenergic, alpha-1
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Saccharin / analogs & derivatives*
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Saccharin / chemical synthesis
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Saccharin / pharmacology
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Structure-Activity Relationship
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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Tamsulosin
Substances
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ADRA1A protein, human
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Adrenergic alpha-1 Receptor Antagonists
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Adrenergic alpha-Antagonists
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Receptors, Adrenergic, alpha-1
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Sulfonamides
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Finasteride
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Terazosin
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Saccharin
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Tamsulosin
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Prazosin