Nafarelin
(Synonyms: 那法瑞林) 目录号 : GC33080
A GNRH agonist
Cas No.:76932-56-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nafarelin is an agonist of gonadotropin-releasing hormone (GNRH).1,2,3 It is a long-acting agent that, after an initial increase in sex hormone levels, decreases the level of circulating gonadotropins and sex hormones. In vivo, nafarelin (0.5-2.0 μg/kg, s.c.) reduces plasma levels of luteinizing hormone and testosterone as well as testicular volume, sperm count, sperm motility, and duration of ejaculation in male dogs.1 Nafarelin (32 μg/animal per day) inhibits estrus in female beagle dogs.2 It also reduces the volume of endometrial tissue in a rat model of endometriosis.3 Formulations containing nafarelin have been used in the treatment of endometriosis and central precocious puberty.
1.Vickery, B.H., McRae, G.I., Briones, W.V., et al.Dose-response studies on male reproductive parameters in dogs with nafarelin acetate, a potent LHRH agonistJ. Androl.6(1)53-60(1985) 2.McRae, G.I., Roberts, B.B., Worden, A.C., et al.Long-term reversible suppression of oestrus in bitches with nafarelin acetate, a potent LHRH agonistJ. Reprod. Fertil.74(2)389-397(1985) 3.Mizutani, T., Sakata, M., and Terakawa, N.Effect of gonadotropin-releasing hormone agonists, nafarelin, buserelin, and leuprolide, on experimentally induced endometriosis in the ratInt. J. Fertil. Menopausal Stud.40(2)106-111(1995)
| Cas No. | 76932-56-4 | SDF | |
| 别名 | 那法瑞林 | ||
| Canonical SMILES | {Glp}-His-Trp-Ser-Tyr-{2-Naph-Ala}-Leu-Arg-Pro-Gly-NH2 | ||
| 分子式 | C66H83N17O13 | 分子量 | 1322.47 |
| 溶解度 | >15.67 mg/mL in DMSO; >51.8 mg/mL in H2O | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7562 mL | 3.7808 mL | 7.5616 mL |
| 5 mM | 0.1512 mL | 0.7562 mL | 1.5123 mL |
| 10 mM | 0.0756 mL | 0.3781 mL | 0.7562 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions
Drugs 1990 Apr;39(4):523-51.PMID:2140979DOI:10.2165/00003495-199039040-00005.
Nafarelin, a synthetic agonist of gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LH-RH); gonadorelin] appears likely to join the other GnRH analogues currently used in a range of conditions reliant on gonadotrophins or sex hormones. With repeated administration, the pituitary becomes desensitised, and gonadotrophin release, and therefore sex hormone synthesis, are inhibited. Nafarelin has proved to be comparable to danazol in the management of women with endometriosis, with fewer potentially harmful adverse effects. Nafarelin has also been used effectively in in vitro fertilisation programmes, and in hirsute women and those with uterine leiomyoma, particularly to induce preoperative fibroid shrinkage. The drug shrinks hypertrophic tissue in men with benign prostatic hyperplasia, although treatment would need to be maintained indefinitely and therefore should probably be reserved for those unsuitable for prostatectomy. Preliminary data suggest that Nafarelin is equivalent to diethylstilbestrol (stilboestrol) in terms of disease-free survival in men with prostate cancer. As a reliable method of contraception, Nafarelin gives unpredictable results in men and the promising results in women may be offset by hypoestrogenic side effects. Nafarelin may join other GnRH agonists which are now routinely used in the management of children with central or combined precocious puberty. Nafarelin is readily and rapidly absorbed following intranasal delivery, and is protected to some extent from enzymatic degradation. The resultant relatively long elimination half-life allows once- or twice-daily administration. Estrogen depletion accounts for the most common side effects associated with Nafarelin, including hot flushes and vaginal dryness, which are mild and tolerable in most patients. Reversible resorption of trabecular bone can occur during Nafarelin therapy, perhaps necessitating cyclical treatment to enable bone mass to recover. Nafarelin, therefore, looks likely to find a role in the treatment of women with endometriosis, and results achieved in other conditions dependent on the pituitary-gonadal axis are promising.
Clinical use of Nafarelin in the treatment of leiomyomas. A review of the literature
J Reprod Med 2000 Jun;45(6):481-9.PMID:10900582doi
Objective: To review the efficacy and safety of Nafarelin in the treatment of leiomyomas. Study design: A literature review of published clinical trials was conducted. Six studies, including a total of 602 patients with leiomyomas, were reviewed. Patients received intranasal Nafarelin, 50-400 micrograms twice daily for three to six months. Vaginal bleeding patterns, leiomyoma and uterine size, surgical conditions and adverse effects were assessed. Results: Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia. The significant reduction in uterine bleeding and amenorrhea resulting from administration of Nafarelin was associated with a rise in mean hemoglobin concentrations. In addition, Nafarelin improved hematologic parameters in women with and without anemia. Nafarelin was well tolerated, although hot flushes were the most commonly reported adverse events. Measured bone mineral density decreased significantly during treatment, although by six to nine months post-treatment, it increased to values not significantly different from baseline. The adverse effects of Nafarelin were generally reversible after treatment withdrawal. Conclusion: Nafarelin treatment of women with symptomatic leiomyomas effectively decreases uterine bleeding; improves hematologic parameters; manages symptoms of menometrorrhagia, dysmenorrhea and pelvic discomfort; reduces uterine and myoma size; and is well tolerated. Reduction in bone mineral density occurs, but levels return to, or near, baseline levels within six months after treatment.
Nafarelin in the management of endometriosis: quality of life assessment
Am J Obstet Gynecol 1992 Feb;166(2):735-9.PMID:1531576DOI:10.1016/0002-9378(92)91705-f.
Quality of life is important when comparing the relative advantages of Nafarelin versus danazol for the treatment of endometriosis. Recent studies have investigated the potential differences between the safety profiles of Nafarelin and danazol and the impact of these profiles on the patient's quality of life. Results show that although these drugs have similar efficacy, they are associated with very different safety profiles. Most notable are the androgenic effects such as weight gain associated with danazol. With Nafarelin, hypoestrogenic side effects, such as hot flashes, are more common. More important, these differences in safety profiles may prove to be relevant to patient satisfaction and compliance with therapy.
Comparison of the pharmacology of Nafarelin and danazol
Am J Obstet Gynecol 1990 Feb;162(2):581-5.PMID:2137975DOI:10.1016/0002-9378(90)90436-b.
The pharmacologic profiles of danazol and Nafarelin differ considerably from each other. Danazol interacts with multiple classes of proteins, whereas the gonadotropin-releasing hormone agonist Nafarelin interacts only with the pituitary gonadotropin-releasing hormone receptor. Differences in the molecular, endocrine, and clinical pharmacologic properties of these agents may provide clues to their varying effects in the management of women with endometriosis.
Prolonged injectable formulation of Nafarelin using in situ gel combination delivery system
Pharm Dev Technol 2018 Feb;23(2):132-144.PMID:28430010DOI:10.1080/10837450.2017.1321662.
The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin-poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin-loaded PHBV NPs were prepared via double emulsion solvent evaporation technique. Box-Behnken Response Surface Methodology was utilized to optimize NPs. Mean particle size, polydispersity index (PDI), entrapment efficiency (EE), and drug loading (DL) of the optimized NPs were measured. Incorporation of Nafarelin within NPs was proven by differential scanning calorimetry (DSC). The combination delivery system (CDS) was prepared by adding Nafarelin-loaded PHBV NPs to sodium alginate/poloxamer 407 solution followed by physical mixing. Morphological properties of Nafarelin-loaded PHBV NPs and CDS were evaluated by SEM. Rheological properties were employed to investigate the effects of alginate concentration on sol-gel transition temperature. The release profile of Nafarelin from both PHBV NPs and CDS were individually assessed. The cumulative release percentage from CDS was significantly lower than Nafarelin released from PHBV NPs. Based on the favorable results in this study, the CDS consisting of sodium alginate/poloxamer 407 loaded with PHBV NPs could be a promising candidate for designing a long-lasting formulation of Nafarelin.