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Histrelin (acetate)

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  • ¥1
  • Cayman
  • 2025年07月15日
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    • 文献和实验
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    合成的GNRH激动剂;与GNRHR结合(在表达人类受体的CHO细胞中Ki=0.2nM);刺激大鼠下丘脑神经垂体系统体外释放催产素和加压素(100nM);100μg的初始剂量可刺激血清LH、FSH和睾酮水平急剧升高(分别为50倍、2.5倍和15倍),而长期治疗会导致恒河猴的LH和FSH反应降低95%。A synthetic GNRH agonist; binds to GNRHR (Ki = 0.2 nM in CHO cells expressing the human receptor); stimulates oxytocin and vasopressin release ex vivo from the isolated rat hypothalamo-neurohypophysial system (100 nM); initial dose of 100 μg stimulates acute increases in LH, FSH, and testosterone serum levels (50-, 2.5-, and 15-fold, respectively), while chronic treatment leads to 95% decreases in LH and FSH responses in rhesus monkeys.

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