TRIPTORELIN 曲普瑞林
CAS 57773-63-4 MFCD00167541
化学结构图
SMILES: CC(C)C[C@H](NC(=O)[C@@H](CC1=CNC2C=CC=CC1=2)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CNC2C=CC=CC1=2)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O
化学属性
| Mol. Formula | C64H82N18O13 |
|---|---|
| Mol. Weight | 1311.45 |
| Appearance | powder |
别名和识别编码
| Chemical Name | TRIPTORELIN |
|---|---|
| Synonym | (D-TRP6)-GONADOTROPIN-RELEASING HORMONE 曲普瑞林 TRIPTORELIN ACETATE TRIPTORELIN, [DTRP6]-LH-RH, AMIDE [D-TRP6]-LUTEINIZING HORMONE-RELEASING HORMONE (HUMAN) (D-TRP6)-LHRH PAMOATE SALT [DTRP6]-LH-RH AMIDE PYR-HIS-TRP-SER-TYR-D-TRP-LEU-ARG-PRO-GLY-NH2 PAMOATE SALT PYROGLU-HIS-TRP-SER-TYR-D-TRP-LEU-ARG-PRO-GLY NH2 醋酸曲普瑞林 [D-Trp6]-Luteinizing hormone releasing hormone TRIPTORELIN (D-TRP6)-LUTEINIZING HORMONE-RELEASING HORMONE [DTRP6]-LUTEINIZING HORMONE-RELEASING HORMONE, AMIDE GLP-HIS-TRP-SER-TYR-D-TRP-LEU-ARG-PRO-GLY-NH2 TRIPTORELIN AMIDE PYR-HIS-TRP-SER-TYR-D-TRP-LEU-ARG-PRO-GLY-NH2 [D-TRP6]-LH-RH (HUMAN) 垂普托雷林 (D-TRP6)-LHRH TRIPTORELINE 曲普瑞林(TRIPTORELIN) (D-TRP6)-LUTEINIZING HORMONE-RELEASING FACTOR PGLU-HIS-TRP-SER-TYR-D-TRP-LEU-ARG-PRO-GLY-NH2 TRIPTORELIN PAMOATE |
| MDL Number | MFCD00167541 |
| CAS Number | 57773-63-4 |
| Chemical Name Translation | 曲普瑞林 |
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分类
- Androgen Modulators, Antitumor Agents, Cancer Research, Cell Biology, Cell Signaling and Neuroscience, LH-RH, Neuropeptides, Peptides and Proteins, Peptides for Cell Biology, Releasing Factors, Therapy Adjuncts, Tumor Growth Regulation
- {SNA} Androgen Modulators, Antitumor Agents, Cancer Research, Cell Biology, Cell Signaling and Neuroscience, LH-RH, Neuropeptides, Peptides and Proteins, Peptides for Cell Biology, Releasing Factors, Therapy Adjuncts, Tumor Growth Regulation
相关文献及参考
- Kadar, T, et al., Behavioral effects of centrally administered LH-RH agonist in rats. Physiol. Behav. 51 , 601-605, (1992) 摘要
- Arencibia, J.M., and Schally, A.V., Luteinizing hormone-releasing hormone as an autocrine growth factor in ES-2 ovarian cancer cell line. Int. J. Oncol. 16 , 1009-1013, (2000) 摘要
- Kim, J.W., et al., Cell cycle arrest in endometrial carcinoma cells exposed to gonadotropin-releasing hormone analog. Gynecol. Oncol. 73 , 368-371, (1999) 摘要
- Emons, G., et al., High affinity binding and direct antiproliferative effects of LHRH analogues in human ovarian cancer cell lines. Cancer Res. 53 , 5439-5446, (1993) 摘要
- Merck 14 ,9748
安全信息
GHS Symbol
- P308+P313
- P201 Obtain special instructions before use. 使用前获取专门指示。
- H360 May damage fertility or the unborn child 可能对生育能力或未出生婴儿造成伤害
- S45 In case of accident or if you feel unwell seek medical advice immediately (show the label where possible) 发生事故时或感觉不适时，立即求医（可能时出示标签）；
- S36/37/39 Wear suitable protective clothing, gloves and eye/face protection 穿戴适当的防护服、手套和眼睛/面保护；
- S22 Do not breathe dust 不要吸入粉尘；
- S53 Avoid exposure - obtain special instructions before use 避免接触，使用前获得特别指示说明；
- R60 May impair fertility 可能降低生殖能力
其他信息
- 抗肿瘤药物:曲普瑞林的活性成分是合成的促性腺激素释放激素(GnRH)的类似物，又称色氨瑞林，达菲林，达必佳，戈那瑞林，是一种抗肿瘤药物，药理作用同戈舍瑞林、布舍瑞林，其结构改良是将天然分子结构中第六个左旋甘氨酸被右旋色氨酸所取代，使其促效作用更为显著及血浆半衷期更长，具有更高的药效力。肌内注射后，最初会刺激垂体释放促黄体生长素 (LH)及促卵泡成熟素(FSH)。当垂体经过长期的刺激后进入不应期，促性腺激素的释放减少，从而使性激素降低至去势水平。上述作用是可逆转的。皮下给药吸收迅速，Tmax为15min，1h达最大效应，缓释制剂肌内注射可维持疗效达28d以上。临床上主要用于治疗子宫内膜异位症、激素依赖性的前列腺癌、乳腺癌、儿童真性性早熟，还可用于辅助生育技术。曲普瑞林的主要不良反应如下：在男性治疗初期可发生泌尿障碍、乳房肿胀及疼痛、骨骼疼痛等，也可出现潮热、性欲减退及阳痿。罕见男子女性型乳房、睾丸萎缩及睡眠紊乱。在儿童治疗第1周会出现女孩少量阴道出血，可用短期的附加治疗纠正。在女性治疗期间可出现潮热、出血或出血斑、阴道干燥、头痛和虚弱等，联合使用促性腺激素时可引起腹腔和(或)盆腔疼痛。由于雌激素的浓度降低至绝经后水平，可引起轻微骨小梁基质丢失。一般在治疗停止后六至九个月均可恢复正常。子宫内膜异位症患者用药后可出现不可逆的闭经。
- MOL 文件:57773-63-4.mol
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