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Abarelix

阿巴瑞克
Mechanism of action:
Abarelix 是一種促性腺激素釋放激素拮抗劑(gonadotropin-releasing hormone antagonist),屬於合成胜肽類(synthetic peptide)。Abarelix 與腦下垂體前葉的促性腺素釋素受體(gonadotropin-releasing hormone receptor)結合,阻止內源性促性腺素釋素與其受體互動,抑制黃體成長激素(LH)與濾泡刺激素(FSH)的分泌。黃體成長激素分泌被抑制後,睪丸的萊迪希細胞(Leydig cell)的睪酮(testosterone)合成明顯下降。
Reference(s):
1. Debruyne FM et al. (2004). Gonadotropin-releasing hormone antagonist in the management of prostate cancer. Rev Urol.
2. Jiang G et al. (2001). GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. J Med Chem.
3. Liu T et al. (2025). BindingDB in 2024: a FAIR knowledgebase of protein-small molecule binding data. Nucleic Acids Res.
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