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鼻腔给予[D-丝氨酸(叔丁基)6,去甘氨酰胺(10)]-促黄体生成激素释放激素乙酰胺对正常女性的黄体溶解作用。

Luteolytic effect of intranasal administration of [D-Ser(TBU)6,DES-Gly-NH2(10)]-luteinizing hormone-releasing hormone ethylamide in normal women.

作者信息

Lemay A, Labrie F, Belanger A, Raynaud J P

出版信息

Fertil Steril. 1979 Dec;32(6):646-51. doi: 10.1016/s0015-0282(16)44412-2.

DOI:10.1016/s0015-0282(16)44412-2
PMID:389676
Abstract

Intranasal administration of two doses of potent agonist of luteinizing hormone (LH)-releasing hormone (LHRH), [D-Ser(TBU)6,des-Gly-NH2(10)]LHRH ethylamide (500 micrograms), a 8 A.M. and 5 P.M. on 1 day between day 4 and 9 following the LH peak in six normal women during two consecutive menstrual cycles shortened the luteal phase from 13.6 +/- 0.3 days to 10.9 +/- 0.3 days (mean shortening, 2.7 days; range, 0.5 to 4.5 days) and reduced plasma progesterone levels to 61.3% +/- 9.2% of control. Hormone changes were followed by daily measurements of plasma LH, follicle-stimulating hormone, 17 beta-estradiol, and progesterone during two pretreatment cycles, two treatment cycles, and two post-treatment cycles. No side effect was observed, and apparently normal cycles occurred immediately after treatment. The present data indicate that the intranasal administration of a potent LHRH agonistic analog can induce luteolysis and control time of occurrence of menses in normal women. This finding opens the possibility of a new and physiologic approach to fertility control.

摘要

在六个正常女性连续两个月经周期中,于促黄体生成素(LH)峰值出现后的第4至9天之间的某一天上午8点和下午5点,经鼻给予两剂促黄体生成素释放激素(LHRH)的强效激动剂[D - 丝氨酸(叔丁基)6,去甘氨酸 - 氨基(10)]LHRH乙酰胺(500微克),使黄体期从13.6±0.3天缩短至10.9±0.3天(平均缩短2.7天;范围为0.5至4.5天),并使血浆孕酮水平降至对照值的61.3%±9.2%。在两个预处理周期、两个治疗周期和两个治疗后周期中,通过每日测量血浆LH、促卵泡生成素、17β - 雌二醇和孕酮来跟踪激素变化。未观察到副作用,且治疗后立即出现明显正常的周期。目前的数据表明,经鼻给予强效LHRH激动剂类似物可诱导黄体溶解并控制正常女性月经发生的时间。这一发现为生育控制开辟了一种新的生理性方法的可能性。

相似文献

1
Luteolytic effect of intranasal administration of [D-Ser(TBU)6,DES-Gly-NH2(10)]-luteinizing hormone-releasing hormone ethylamide in normal women.鼻腔给予[D-丝氨酸(叔丁基)6,去甘氨酰胺(10)]-促黄体生成激素释放激素乙酰胺对正常女性的黄体溶解作用。
Fertil Steril. 1979 Dec;32(6):646-51. doi: 10.1016/s0015-0282(16)44412-2.
2
Luteolytic activity of LHRH and [D-Ser(TBU)6, des-Gly-NH2(10)]LHRH ethylamide: a new and physiological approach to contraception in women.促黄体生成素释放激素(LHRH)和[D-丝氨酸(叔丁基)6,去甘氨酰胺(10)]LHRH乙酰胺的溶黄体活性:一种新型女性避孕生理方法
Int J Fertil. 1980;25(3):203-12.
3
Sensitivity of pituitary and corpus luteum responses to single intranasal administration of (D-ser[TBU]6-des-gly-NH2(10)) luteinizing hormone-releasing hormone ethylamide (Buserelin) in normal women.正常女性垂体和黄体对单次鼻内给予(D-丝氨酸[TBU]6-去甘氨酰胺(10))促黄体生成素释放激素乙酰胺(布舍瑞林)反应的敏感性。
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Possible luteolytic effects of luteinizing hormone-releasing hormone in normal women.促黄体生成激素释放激素对正常女性可能的溶黄体作用。
Fertil Steril. 1979 Jan;31(1):29-34. doi: 10.1016/s0015-0282(16)43755-6.
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Inhibition of ovulation during discontinuous intranasal luteinizing hormone-releasing hormone agonist dosing in combination with gestagen-induced bleeding.在间断经鼻给予促黄体生成素释放激素激动剂并联合孕激素诱导出血期间对排卵的抑制作用。
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Gonadotroph and corpus luteum responses to two successive intranasal doses of a luteinizing hormone-releasing hormone agonist at different days after the midcycle luteinizing hormone surge.在月经周期中期促黄体生成素高峰后的不同天数,促性腺激素细胞和黄体对连续两次鼻内给予促黄体生成素释放激素激动剂的反应。
Fertil Steril. 1983 May;39(5):661-7. doi: 10.1016/s0015-0282(16)47062-7.
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Gonadotropins and estradiol responses to single intranasal or subcutaneous administration of a luteinizing hormone-releasing hormone agonist in the early follicular phase.卵泡早期单次经鼻或皮下注射促黄体生成素释放激素激动剂后促性腺激素和雌二醇的反应
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Effect of postovulatory treatment with a luteinizing hormone-releasing hormone analog on the plasma level of progesterone in women.促黄体生成素释放激素类似物排卵后治疗对女性血浆孕酮水平的影响。
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Suppression of luteal function by a luteinizing hormone-releasing hormone antagonist during the early luteal phase in the stumptailed macaque monkey and the effects of subsequent administration of human chorionic gonadotropin.黄体生成素释放激素拮抗剂对短尾猕猴黄体期早期黄体功能的抑制作用及随后给予人绒毛膜促性腺激素的影响
Endocrinology. 1987 Aug;121(2):612-8. doi: 10.1210/endo-121-2-612.

引用本文的文献

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Endocr Rev. 2018 Oct 1;39(5):593-628. doi: 10.1210/er.2017-00236.
2
Clinical parameters of ovarian hyperstimulation syndrome following different hormonal triggers of oocyte maturation in IVF treatment.不同激素触发卵母细胞成熟在 IVF 治疗中对卵巢过度刺激综合征的临床参数。
Clin Endocrinol (Oxf). 2018 Jun;88(6):920-927. doi: 10.1111/cen.13569. Epub 2018 Mar 6.
3
Effect of chronic treatment with [D-Ala6, des-Gly-NH210]LHRH ethylamide on ovarian histology in the rat.
[D-丙氨酸6,去甘氨酰胺10]促黄体激素释放激素乙酰胺长期治疗对大鼠卵巢组织学的影响。
Cell Tissue Res. 1982;227(1):213-9. doi: 10.1007/BF00206342.
4
GnRH and its analogues. Current therapeutic applications and new prospects.促性腺激素释放激素及其类似物。当前的治疗应用与新前景。
Drugs. 1984 Mar;27(3):187-93. doi: 10.2165/00003495-198427030-00001.
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Similar luteinizing hormone-releasing hormone binding sites in rat anterior pituitary and ovary.大鼠垂体前叶和卵巢中类似的促黄体生成激素释放激素结合位点。
Proc Natl Acad Sci U S A. 1980 Sep;77(9):5567-71. doi: 10.1073/pnas.77.9.5567.
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GnRH agonists and antagonists. Current clinical status.促性腺激素释放激素激动剂和拮抗剂。当前临床状况。
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Buserelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical profile.布舍瑞林。对其药效学和药代动力学特性以及临床概况的综述。
Drugs. 1990 Mar;39(3):399-437. doi: 10.2165/00003495-199039030-00007.