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化学名
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(1S,3aS,3bS,5aR,9aR,9bS,11aS)-N-[2,5-bis(trifluoromethyl)phenyl]-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide
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分子式
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C27H30F6N2O2
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详细内容
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Dutasteride (Avodart) is an inhibitor of dual 5-alpha-reductase for treating benign prostatic hyperplasia (BPH).
Dutasteride has been reported to inhibit conversion of 3H-testosterone to 3H-DHT by more than 99% in LNCaP cells. Dutasteride strongly reduces growth, proliferation, and viability of LNCaP cells as well. Dutasteride increased the enzymatic activities of caspase 7 and caspase 8 dose-dependently at 48 hours, providing functional significance and confirming that the apoptotic and survival pathways are being activated by dutasteride treatment in LNCaP cells [1].
In vivo, dutasteride, which inhibits both 5αR1/5αR2, is efficacious in blocking prostate cancer development or progression in C57BL/6 TRAMP x FVB mice [2].
References:
[1] Schmidt LJ1, Murillo H, Tindall DJ. Gene expression in prostate cancer cells treated with the dual 5 alpha-reductase inhibitor dutasteride. J Androl. 2004 Nov-Dec;25(6):944-53.
[2] Opoku-Acheampong AB1, Unis D, Henningson JN, Beck AP, Lindshield BL.Preventive and therapeutic efficacy of finasteride and dutasteride in TRAMP mice. PLoS One. 2013 Oct 18;8(10):e77738. doi: 10.1371/journal.pone.0077738. eCollection 2013.
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