Nafarelin (acetate)
目录号 : GC44310
A GNRH agonist
Cas No.:76932-60-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nafarelin is an agonist of gonadotropin-releasing hormone (GNRH). 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. Nafarelin (32 μg/animal per day) inhibits estrus in female beagle dogs. It also reduces the volume of endometrial tissue in a rat model of endometriosis. Formulations containing nafarelin have been used in the treatment of endometriosis and central precocious puberty.
| Cas No. | 76932-60-0 | SDF | |
| Canonical SMILES | O=C(N[C@@H](CO)C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](CC2=CC(C=CC=C3)=C3C=C2)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N4CCC[C@H]4C(NCC(N)=O)=O)=O)=O)=O)=O)=O)[C@@H](NC([C@@H](NC([C@@H]5CCC(N5)=O)=O)CC6=CNC=N6)=O)CC7=CNC8=C7C=CC=C8.OC(C)=O | ||
| 分子式 | C66H83N17O13•XC2H4O2 | 分子量 | 1322.5 |
| 溶解度 | DMSO: Slightly Soluble,Methanol: Slightly Soluble,Water: Slightly Soluble | 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 | 0.7561 mL | 3.7807 mL | 7.5614 mL |
| 5 mM | 0.1512 mL | 0.7561 mL | 1.5123 mL |
| 10 mM | 0.0756 mL | 0.3781 mL | 0.7561 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 vs. leuprolide acetate depot for endometriosis. Changes in bone mineral density and vasomotor symptoms. Nafarelin Study Group
J Reprod Med 1997 Jul;42(7):413-23.PMID:9252932doi
Objective: To compare intranasal Nafarelin and intramuscular leuprolide acetate (LA) depot in the management of endometriosis. Study design: A multicenter, prospective, randomized, double-placebo, double-blind study was conducted on subjects who had symptoms and signs of endometriosis and bone mineral density (BMD) within the age-appropriate normal range. For 6 months, 99 subjects received Nafarelin, 200 micrograms twice daily, and placebo injections once monthly; 93 subjects received LA depot injections, 3.75 mg once monthly, and placebo nasal spray, twice daily. Subjects were followed throughout treatment and for six months after treatment. The main outcome measures were changes in endometriosis symptoms and signs, BMD measurements, subject-reported and objectively measured hot flushes and circulating estradiol concentrations. Results: Nafarelin was as effective as LA depot in alleviating symptoms and signs of endometriosis. LA depot recipients lost significantly more BMD, had more days with subjective hot flushes and more objectively measured hot flushes than did Nafarelin recipients. In the Nafarelin group, estradiol levels were consistently higher than in the leuprolide depot group, with significant differences by month 3 of dosing. Conclusion: Nafarelin and LA depot were equally effective despite higher estradiol levels in Nafarelin recipients. Nafarelin-treated subjects lost less BMD, had fewer days with hot flushes and had fewer objectively measured hot flushes.
Disposition of Nafarelin acetate, a potent agonist of luteinizing hormone-releasing hormone, in rats and rhesus monkeys
Drug Metab Dispos 1985 Sep-Oct;13(5):560-5.PMID:2865103doi
Nafarelin acetate, [6-(3-(2-naphthyl)-D-Ala)]-luteinizing hormone-releasing hormone (LHRH), is a synthetic LHRH agonist. In the suppression of estrus in female rats, Nafarelin acetate was about 200 times as potent as LHRH. We have studied the distribution and excretion of radiolabeled Nafarelin acetate administered iv to rats and rhesus monkeys and have also compared the pharmacokinetics of Nafarelin acetate to LHRH in these two species. Distribution of a single 100-micrograms dose [14C]Nafarelin acetate into tissues in male rats was rapid and of the 13 tissues assayed, highest concentrations of radioactivity were observed in the kidneys, liver, and intestines. The urine to feces ratio of nafarelin-associated 14C was 4:1 in rhesus monkeys and 1:3 in rats. Nafarelin acetate and LHRH given iv to female rhesus monkeys in approximately equimolar doses (6.5 nmol/kg) had terminal plasma t1/2 values of 120 min and 33 min, and systemic clearance values of 2.7 ml/min/kg and 31.4 ml/min/kg, respectively. In female rats, the plasma t1/2 was 33.6 min for Nafarelin acetate and 6.7 min for LHRH, and the systemic clearance values for Nafarelin acetate and LHRH were 12.0 ml/min/kg and 57.6 ml/min/kg, respectively, after approximately equimolar doses.
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.
A prospective randomized comparison of routine buserelin acetate and a decreasing dosage of Nafarelin acetate with a low-dose gonadotropin-releasing hormone agonist protocol for in vitro fertilization and intracytoplasmic sperm injection
Fertil Steril 2001 Sep;76(3):532-7.PMID:11532477DOI:10.1016/s0015-0282(01)01977-x.
Objective: To compare the efficacy of a draw-back Nafarelin acetate protocol with routine buserelin acetate administration for in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI). Design: Prospective clinical study. Setting: Mie University School of Medicine, Tsu, Mie, Japan. Patient(s): One hundred sixty-nine women treated with IVF and 183 women treated with ICSI. Intervention(s): Nafarelin acetate and buserelin acetate in ovarian hyperstimulation in IVF and ICSI were administered. Main outcome measure(s): The concentrations of estradiol (E(2)), FSH, LH, gonadotropin dosages; the number of oocytes retrieved, oocytes fertilized, and embryos; and pregnancy rates. Result(s): A prospective study was conducted with 44 cycles for 34 couples with Nafarelin acetate (group 1) and 47 cycles for 40 couples with buserelin acetate (group 2) with a long IVF protocol; 68 cycles for 46 couples with Nafarelin acetate (group 3) and 56 cycles for 39 couples with buserelin acetate (group 4) with a short IVF protocol; 39 cycles for 32 couples with Nafarelin acetate (group 5) and 50 cycles for 30 couples with buserelin acetate (group 6) with a long ICSI protocol; and 87 cycles for 60 couples with Nafarelin acetate (group 7) and 81 cycles for 61 couples with buserelin acetate (group 8) with a short ICSI protocol. Patients were randomized to receive either full-dose Nafarelin acetate (200 microg b.i.d.) treatment for 7 days followed by half-dose Nafarelin acetate (200 microg daily) or buserelin acetate (300 microg t.i.d.). There were no statistically significant differences in baseline concentrations of E(2) and FSH, concentrations of E(2), P4, FSH, LH on hCG administration, gonadotropin dosage, the number of oocytes retrieved and embryos transferred, or pregnancy rates between groups 1 and 2, groups 3 and 4, groups 5 and 6, and groups 7 and 8. Conclusion(s): Full-dose Nafarelin acetate treatment for 7 days followed by half-dose Nafarelin acetate ("draw-back" protocol) is an effective new protocol for IVF and ICSI.
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.