Neuropeptide S (human) (acetate)
(Synonyms: NPS) 目录号 : GC47769A neuropeptide NSPR agonist
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
Neuropeptide S is a neuropeptide expressed in the brain, primarily in glutamatergic neurons near the locus coeruleus and in the trigeminal sensory nucleus, as well as in neurons of the lateral parabrachial nucleus in rat brain.1 It is an agonist of the neuropeptide S receptor (NPSR) with an EC50 value of 9.4 nM for the human peptide to induce intracellular calcium mobilization in HEK293 cells expressing the human receptor.2 Neuropeptide S (0.1-1 nmol), administered either intracerebroventricularly or into the paraventricular nucleus (PVN) of the hypothalamus, increases plasma adrenocorticotropic hormone (ACTH) and corticosterone levels in rats.3 Administration into the PVN also decreases food intake in the hour following doses of 0.1, 0.3, and 1 nmol. Neuropeptide S decreases anxiety-like and fear behaviors in rodents, decreasing defensive burying in rats, increasing the time mice spend in the open arms of the elevated plus maze, and enhancing contextual fear extinction in mice.4,5
1.Xu, Y.-L., Gall, C.M., Jackson, V.R., et al.Distribution of neuropeptide S receptor mRNA and neurochemical characteristics of neuropeptide S-expressing neurons in the rat brainJ. Comp. Neurol.500(1)84-102(2007) 2.Xu, Y.-L., Reinscheid, R.K., Huitron-Resendiz, S., et al.Neuropeptide S: A neuropeptide promoting arousal and anxiolytic-like effectsNeuron43(4)487-497(2004) 3.Smith, K.L., Patterson, M.L., Dhillo, W.S., et al.Neuropeptide S stimulates the hypothalamo-pituitary-adrenal axis and inhibits food intakeEndocrinology147(7)3510-3518(2006) 4.Vitale, G., Filaferro, M., Ruggieri, V., et al.Anxiolytic-like effect of neuropeptide S in the rat defensive buryingPeptides29(12)2286-2291(2008) 5.JÜngling, K., Seidenbecher, T., Sosulina, L., et al.Neuropeptide S-mediated control of fear expression and extinction: Role of intercalated GABAergic neurons in the amygdalaNeuron59(2)298-310(2008)
| Cas No. | N/A | SDF | |
| 别名 | NPS | ||
| Canonical SMILES | [H]N[C@@H](CO)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(N)=O)C(NCC(N[C@@H](C(C)C)C(NCC(N[C@]([C@@H](C)O)([H])C(NCC(N[C@H](C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@]([C@@H](C)O)([H])C(N[C@@H](CO)C(N[C@H](C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@@H](CCCCN)C(N[C@@H](CO)C(O)=O)=O)=O)C)=O)=O)=O)CC1=CC=CC=C1)=O)=O)=O)=O)=O)CCSC)=O)=O)=O)=O)=O)=O)=O)=O)CC2=CC=CC=C2)=O.CC(O)=O | ||
| 分子式 | C93H155N31O28S.XC2H4O2 | 分子量 | 2187.5 |
| 溶解度 | Water: 1 mg/ml | 储存条件 | Store at -20°C; protect from light |
| 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 | 0.4571 mL | 2.2857 mL | 4.5714 mL |
| 5 mM | 0.0914 mL | 0.4571 mL | 0.9143 mL |
| 10 mM | 0.0457 mL | 0.2286 mL | 0.4571 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。
Leuprolide acetate: a drug of diverse clinical applications
Expert Opin Investig Drugs 2007 Nov;16(11):1851-63.PMID:17970643DOI:10.1517/13543784.16.11.1851.
Leuprolide acetate is a synthetic nonapeptide that is a potent gonadotropin-releasing hormone receptor (GnRHR) agonist used for diverse clinical applications, including the treatment of prostate cancer, endometriosis, uterine fibroids, central precocious puberty and in vitro fertilization techniques. As its basic mechanism of action, leuprolide acetate suppresses gonadotrope secretion of luteinizing hormone and follicle-stimulating hormone that subsequently suppresses gonadal sex steroid production. In addition, leuprolide acetate is presently being tested for the treatment of Alzheimer's disease, polycystic ovary syndrome, functional bowel disease, short stature, premenstrual syndrome and even as an alternative for contraception. Mounting evidence suggests that GnRH agonist suppression of serum gonadotropins may also be important in many of the clinical applications described above. Moreover, the presence of GnRHR in a multitude of non-reproductive tissues including the recent discovery of GnRHR expression in the hippocampi and cortex of the human brain indicates that GnRH analogs such as leuprolide acetate may also act directly via tissue GnRHRs to modulate (brain) function. Thus, the molecular mechanisms underlying the therapeutic effect of GnRH analogs in the treatment of these diseases may be more complex than originally thought. These observations also suggest that the potential uses of GnRH analogs in the modulation of GnRH signaling and treatment of disease has yet to be fully realized.
Hormonal drugs for the treatment of endometriosis
Curr Opin Pharmacol 2022 Dec;67:102311.PMID:36279764DOI:10.1016/j.coph.2022.102311.
In the past, the primary approach for the treatment of endometriosis was represented by surgery; however, after the introduction of non-invasive diagnosis of endometriosis with the development of imaging technologies, medical treatment became the preferred approach, particularly in young patients. Hormonal drugs, by blocking menstruation, are the most effective for the treatment of endometriosis-related pain, independently of phenotype (ovarian, deep, or superficial endometriosis). Gonadotropin-releasing hormone analogs and oral antagonists act on hypothalamus-pituitary-ovary axis inducing iatrogenic menopause, thus reducing dysmenorrhea and all pain symptoms. The side effects, such as hot flushes and bone loss, may be reduced by an add-back therapy. However, the cost in terms of women's health remains high in view of a long-term treatment. Progestins are considered the first-line treatment, highly effective, and with reduced side effects. In addition to the well-known and largely used Norethisterone acetate and Medroxyprogesterone acetate, recently Dienogest has become one of the most used drugs in all endometriosis phenotypes for long-term treatment. Besides, Intrauterine levornogestrel or subcutaneous etonogestrel are valid alternative for long-term treatment.
Phase 3 Trial of a Small-volume Subcutaneous 6-Month Duration Leuprolide acetate Treatment for Central Precocious Puberty
J Clin Endocrinol Metab 2020 Oct 1;105(10):e3660-e3671.PMID:32738042DOI:10.1210/clinem/dgaa479.
Context: Gonadotropin-releasing hormone agonists (GnRHas) are standard of care for central precocious puberty (CPP). A 6-month subcutaneous injection has recently been approved by the Food and Drug Administration. Objective: Determine efficacy, pharmacokinetics, and safety of 6-month 45-mg subcutaneous leuprolide acetate for CPP. Design: Phase 3 multicenter, open-label, single-arm study. Setting: 25 sites in 6 countries. Subjects: 64 GnRHa-naïve children with CPP (age: 7.5 ± 0.1 years) received study drug: 59 completed the study. Intervention(s): 2 doses of 45-mg subcutaneous leuprolide acetate (0.375 mL) at 0 and 24 weeks; children were followed for 48 weeks. Main outcome measure(s): Percentage of children with serum luteinizing hormone (LH) <4 IU/L 30 minutes following GnRHa stimulation at week 24. Results: 54/62 (87%) children achieved poststimulation LH <4 IU/L at week 24; 49/56 (88%) girls and 1/2 boys maintained peak LH <4 IU/L at week 48. Mean growth velocity decreased from 8.9 cm/year at week 4 to 6.0 cm/year at week 48. Mean bone age was advanced 3.0 years beyond chronological age at screening and 2.7 years at week 48. Breast pubertal stage regressed or was stable in 97% of girls and external genitalia development regressed in both boys. Adverse events were mild and did not cause treatment discontinuation. Conclusions: A small volume of 45-mg subcutaneous leuprolide acetate administered at a 6-month interval effectively suppressed pubertal hormones and stopped or caused regression of pubertal progression. This long-acting GnRHa preparation of leuprolide acetate is a new, effective, and well-tolerated therapy for children with CPP.
Acute acetate administration increases endogenous opioid levels in the human brain: A [11C]carfentanil molecular imaging study
J Psychopharmacol 2021 May;35(5):606-610.PMID:33406950DOI:10.1177/0269881120965912.
Introduction: A recent study has shown that acetate administration leads to a fourfold increase in the transcription of proopiomelanocortin (POMC) mRNA in the hypothalamus. POMC is cleaved to peptides, including β-endorphin, an endogenous opioid (EO) agonist that binds preferentially to the µ-opioid receptor (MOR). We hypothesised that an acetate challenge would increase the levels of EO in the human brain. We have previously demonstrated that increased EO release in the human brain can be detected using positron emission tomography (PET) with the selective MOR radioligand [11C]carfentanil. We used this approach to evaluate the effects of an acute acetate challenge on EO levels in the brain of healthy human volunteers. Methods: Seven volunteers each completed a baseline [11C]carfentanil PET scan followed by an administration of sodium acetate before a second [11C]carfentanil PET scan. Dynamic PET data were acquired over 90 minutes, and corrected for attenuation, scatter and subject motion. Regional [11C] carfentanil BPND values were then calculated using the simplified reference tissue model (with the occipital grey matter as the reference region). Change in regional EO concentration was evaluated as the change in [11C]carfentanil BPND following acetate administration. Results: Following sodium acetate administration, 2.5-6.5% reductions in [11C]carfentanil regional BPND were seen, with statistical significance reached in the cerebellum, temporal lobe, orbitofrontal cortex, striatum and thalamus. Conclusions: We have demonstrated that an acute acetate challenge has the potential to increase EO release in the human brain, providing a plausible mechanism of the central effects of acetate on appetite in humans.
Histrelin Hydrogel Implant--Valera: Histrelin implant, LHRH-Hydrogel implant, RL 0903, SPD 424
Drugs R D 2005;6(1):53-5.PMID:15801868DOI:10.2165/00126839-200506010-00007.
Valera Pharmaceuticals, formerly Hydro Med Sciences, is developing a once-yearly Histrelin Hydrogel Implant [Histrelin implant, LHRH-Hydrogel implant, RL 0903, SPD 424, Vantas], a subcutaneous (s.c.) reservoir device capable of long-term delivery of histrelin at constant release rates for the treatment of prostate cancer. Histrelin is a luteinising hormone-releasing hormone agonist (LHRH). A different formulation of the LHRH implant is currently in development for the treatment of central precocious puberty (CPP). On 4 September 2003, Hydro Med Sciences announced that it had changed its name to Valera Pharmaceuticals. Shire Pharmaceuticals had an option to market and distribute the histrelin implant outside the US, but in a realigned agreement announced in January 2002, Shire stated that HydroMed (now Valera) would be responsible for concluding the phase III studies, filing for regulatory approval and producing the implant, while also gaining marketing rights in the US. Shire has no further involvement in development, but retains an option to market and distribute the product outside the US. The product is available for rest-of-the-world licensing through Valera Pharmaceuticals' business development division. Paladin Labs has received the exclusive rights for the sale and marketing of histrelin hydrogel implant in Canada. Valera Pharmaceuticals will have the responsibility for manufacturing and completing development of the product. In July 2004, Paladin announced it had filed for regulatory approval with Health Canada for the treatment of prostate cancer. Phase III trials have been conducted and initially involved two open-labelled, randomised, parallel studies that compared the hydrogel implant with the active comparators, leuprorelin acetate 22.5 mg depot (TAP Pharmaceutical's Lupron Depot) and a 3-month implant of goserelin acetate (Astra Zeneca's Zoladex). However, because of financial constraints, HydroMed discontinued recruitment in a phase II European study and could not rationalise keeping the comparator arm of the phase III study. The US FDA then gave permission to continue the US part of the programme without the comparator arm, but with appropriate increases in the patient sample size. Patient enrolment in the phase III trial (US and Canada) was completed in July 2002. Valera Pharmaceuticals believes the product may have advantages over standard prostate cancer treatments including reduced costly surgical procedures, lower dosing, increased patient compliance and peace-of-mind, as well as potentially less cost to the patient. The phase III studies were completed in the second half of 2003.CPP arises from the increased release by the pituitary gland hormone gonadotropins and is characterised by an early onset of sexual development in pre-adolescents. Currently, the treatment of CPP involves injections of synthetic gonadotropic hormone-releasing factor agonists such as Supprelin (histrelin acetate) and TAP Pharmaceutical's Lupron Depot-Red (leuprolide acetate) every 28 days, a potentially painful procedure. This treatment inhibits pituitary release of gonadotropins. Valera's histrelin implant is a compact, removable subcutaneous implant that can be applied under a local anaesthetic in doctor's surgery.