Estudio de calidad de vida en pacientes con hiperplasia benigna de próstata en tratamiento con silodisina

A series of indoline and indole derivatives were designed, synthesized, and evaluated as selective α1A-adrenergic receptor (α1A-AR) antagonists for the treatment of benign prostatic hyperplasia (BPH). In this study, two highly selective and potent α1A-AR antagonists, compounds (R)-14r (IC50 = 2.7 nM, α1B/α1A = 640.1, α1D/α1A = 408.2) and (R)-23l (IC50 = 1.9 nM, α1B/α1A = 1506, α1D/α1A = 249.6), which exhibited similar activities and better selectivities in cell-based calcium assays as compared with the marketed drug silodosin (IC50 = 1.9 nM, α1B/α1A = 285.9, α1D/α1A = 14.4), were identified. In the functional assays with isolated rat tissues, compounds (R)-14r and (R)-23l also showed high potency and uroselectivity. Most importantly, (R)-14r and (R)-23l can significantly decrease the micturition frequency and increase the mean voided volume of the BPH rats in a dose-dependent manner, making them worthy of further investigation for the development of anti-BPH agents.

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Estudio de calidad de vida en pacientes con hiperplasia benigna de próstata en tratamiento con silodisina

Cited by 2 publications

References 20 publications

Using EQ-5D-3L and OAB-5D to assess changes in the health-related quality of life of men with lower urinary tract symptoms associated with benign prostatic hyperplasia

Using EQ-5D-3L and OAB-5D to assess changes in the health-related quality of life of men with lower urinary tract symptoms associated with benign prostatic hyperplasia

Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selective α_1A-Adrenoceptor Antagonists

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Estudio de calidad de vida en pacientes con hiperplasia benigna de próstata en tratamiento con silodisina

Cited by 2 publications

References 20 publications

Using EQ-5D-3L and OAB-5D to assess changes in the health-related quality of life of men with lower urinary tract symptoms associated with benign prostatic hyperplasia

Using EQ-5D-3L and OAB-5D to assess changes in the health-related quality of life of men with lower urinary tract symptoms associated with benign prostatic hyperplasia

Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selective α1A-Adrenoceptor Antagonists

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Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selective α_1A-Adrenoceptor Antagonists