A practical reference on 胃饥饿素受体: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
This page was last updated on 2025-08-07 and is reviewed periodically as new material appears.
Ipamorelin 是一种合成五肽，序列为 Aib-His-D-2-Nal-D-Phe-Lys-NH2，分子式 C38H49N9O5，游离碱分子量约 711.85 g/mol。它属于生长激素促分泌素（GHS）家族，作用靶点是胃饥饿素受体 GHS-R1a。该化合物由诺和诺德的研究团队在二十世纪九十年代末报道，设计目标是提高对生长激素释放的选择性。C 端酰胺化与 N 端 Aib 残基是两个用于抵抗肽酶降解的结构特征。
在 GHS 家族中，早期肽类如 GHRP-6 与 GHRP-2 会同时促进生长激素、皮质醇与催乳素的释放，并明显增加食欲。Ipamorelin 在动物与早期人体研究中表现出对生长激素释放的相对选择性，对上述其他激素的影响较小。这种差异通常归因于受体结合模式与下游信号偏向的不同，而完整的分子解释仍有待补充。需要区分的是，选择性是研究观察中的相对程度，并非绝对界限。
从用途定位看，ipamorelin 目前主要以研究用肽的身份被讨论，未见主要药品监管机构将其批准为治疗药物。市售材料通常标注仅供研究使用，不得用于人体或诊断程序。文献中它常与生长激素促分泌素、GHS-R1a 激动剂、胃饥饿素拟似物等表述并列出现。既有研究的样本量普遍偏小，因此对其效应强度与一致性的描述应保持谨慎。
At the receptor level, ipamorelin binds GHS-R1a and triggers signaling through Gq-coupled pathways. Activation leads to calcium release and downstream effects in pituitary somatotroph cells. These events promote the release of growth hormone into circulation. The response depends on the presence of the receptor and on the physiological state of the animal or tissue studied. Because the receptor is also found in other tissues, effects beyond the pituitary have been examined in laboratory models, though the extent of those effects remains an area of ongoing study.
One distinguishing feature reported in animal studies is selectivity. Ipamorelin stimulated growth hormone release with limited elevation of adrenocorticotropic hormone or cortisol compared with earlier secretagogues such as GHRP-6. This pattern has been described as more selective for the growth hormone axis. The finding comes mainly from preclinical work, and the degree to which it holds across species and doses is not fully settled. Reports also describe effects on gastric motility in animal models, suggesting activity outside the pituitary, though the clinical relevance of this observation is uncertain.
Ipamorelin is a synthetic pentapeptide that acts on the growth hormone secretagogue receptor, also known as the ghrelin receptor. Its sequence contains five amino acid residues, including a non-natural residue that increases stability against enzymatic breakdown. The compound was developed in the 1990s as part of research into small peptides that stimulate pituitary hormone release. Unlike larger protein hormones, it can be produced by solid-phase peptide synthesis and characterized by standard analytical methods.
| Property | Value | Notes |
|---|---|---|
| 分子式 | C38H49N9O5 | 五肽，C 端酰胺化 |
| 分子量 | 约 711.85 g/mol | 游离碱形式 |
| 外观 | 白色至类白色冻干粉 | 研究用材料的常见形态 |
| 溶解性 | 溶于水及 DMSO 等极性溶剂 | 建议现配现用 |
| 储存温度 | -20 °C 或更低 | 干燥、避光、限制冻融次数 |
Selectivity is the property most often attached to this peptide. Published animal and early human studies record increases in growth hormone release after administration, with adrenocorticotropic hormone and cortisol responses remaining small by comparison. Effects on appetite-related pathways also appear weaker than those reported for several earlier secretagogues. Reviews that compare members of the growth hormone secretagogue family cite these findings frequently, though the receptor-level explanation for the selectivity continues to be debated rather than settled.
Ipamorelin is a synthetic pentapeptide classified as a growth hormone secretagogue. Its sequence, Aib-His-D-2-Nal-D-Phe-Lys-NH2, combines three non-proteinogenic residues with a C-terminal amide. The N-terminal aminoisobutyric acid unit and the two aromatic D-amino acids distinguish it from peptides assembled only from standard L-amino acids. Its formula is C38H49N9O5, corresponding to an average mass near 711.9 Da. At neutral pH the molecule carries a net positive charge, a property that shapes its behaviour in chromatographic and electrophoretic systems.
The compound was developed at Novo Nordisk during the 1990s as part of a programme seeking secretagogues with improved selectivity. It was described in the peer-reviewed literature in 1998 alongside related pentapeptides from the same series. Investigators advanced it because it raised growth hormone output in animal models while leaving other pituitary hormones comparatively unaffected. The development code NNC 26-0161 appears in earlier reports, and ipamorelin later became the common designation in published work.
现有文献多来自小规模、短期的研究，涉及生长激素缺乏、术后肠麻痹等方向。长期使用是否导致受体脱敏，以及重复给药后效应是否衰减，仍属开放问题。不同研究之间的剂量、给药途径和受试者特征差异较大，因此结论外推需谨慎。关于临床获益的确切证据尚不充分，需要更大规模的对照试验来澄清。
Ipamorelin 是一种合成五肽，在 20 世纪 90 年代被报道为生长激素促分泌剂。其结构基于胃饥饿素受体激动剂的设计思路，但并非天然激素。早期药理学研究显示，它可刺激垂体释放生长激素，而对应激激素轴的影响相对较小。该化合物常被用作研究生长激素调节通路的工具分子。
== Medical uses == EMP is indicated, in the United States, for the palliative treatment of metastatic and/or progressive prostate cancer, whereas in the United Kingdom it is indicated for the treatment of unresponsive or relapsing prostate cancer. The medication is usually reserved for use in hormone-refractory cases of prostate cancer, although it has been used as a first-line monotherapy as well. Response rates with EMP in prostate cancer are said to be equivalent to conventional high-dose estrogen therapy. Due to its relatively severe side effects and toxicity, EMP has rarely been used in the treatment of prostate cancer. This is especially true in Western countries today. As a result, and also due to the scarce side effects of gonadotropin-releasing hormone modulators (GnRH modulators) like leuprorelin, EMP was almost abandoned. However, encouraging clinical research findings resulted in renewed interest of EMP for the treatment of prostate cancer. EMP has been used at doses of 140 to 1,400 mg/day orally in the treatment of prostate cancer. However, oral EMP is most commonly used at a dose of 560 to 640 mg/day (280–320 mg twice daily). The recommended dosage of oral EMP in the Food and Drug Administration (FDA) label for Emcyt is 14 mg per kg of body weight (i.e., one 140 mg oral capsule for each 10 kg or 22 lbs of body weight) given in 3 or 4 divided doses per day. The label states that most patients in studies of oral EMP in the United States have received 10 to 16 mg per kg per day. This would be about 900 to 1,440 mg/day for a 90-kg or 200-lb man.
=== Metastasis === CAF have been found to promote tumour metastasis in numerous ways. Firstly, they may alter gene expression and have been found to upregulate specific genes involved in pro-tumorigenic pathways including heat shock factor 1 (HSF1). They can also interfere with the function of tumour suppressor genes, such as Tumour protein p53, leading to higher rates of cell proliferation due to the loss of control of the cell cycle. Additionally, CAF have the ability to break down proteins in the extracellular matrix and basement membranes leading to disruption to the normal structure allowing cells to move away from their primary region. The group of proteins known as the matrix metalloproteinases are key to this process. CAF also direct the movement of neoplastic cells by using the Rho-dependent signaling pathway to create tracks for these cells in the matrix.
=== CD38 === CD38 is an enzyme that triggers inflammatory responses and type II CD38 contains an ecto-NADase or extracellular NADase, whereas type II CD38 contains an intracellular cADPR. CD38 consumes NAD, which can produce second messengers that help regulate immune activity. Cells that are programmed for cell death or apoptosis releases NAD+, and type II CD38 help recycle the extracellular NAD+ released from apoptosis, where both products of NADase, ADP-ribose and nicotinamide, can be used to resynthesize NAD+ via the NAD+ synthesis pathway. ADP-ribose must be converted to adenosine in order to enter the NAD+ synthesis pathway, where ADP-ribose first gets converted to AMP and then AMP gets converted to adenosine via non-classical adenosine generational pathway. The other product nicotinamide is membrane permeable, which allows the molecule to re-enter the NAD synthesis pathway more easily. CD38 NADase is also found in tissues and cells other than T cells, and CD38 is one of the main forms of NADase activity in mammals.
The Romanian revolution (Romanian: Revoluția română) was a period of violent civil unrest in the Socialist Republic of Romania during December 1989 as a part of the revolutions of 1989 that occurred in several countries around the world, primarily within the Eastern Bloc. The Romanian revolution started in the city of Timișoara and soon spread throughout the country, ultimately culminating in the drumhead trial and execution of longtime Romanian Communist Party (PCR) General Secretary Nicolae Ceaușescu and his wife Elena, and the end of 42 years of Communist rule in Romania. It was also the last removal of a Marxist–Leninist government in a Warsaw Pact country during the events of 1989, and the only one that violently overthrew a country's leadership and executed its leader; according to estimates, over one thousand people died and thousands more were injured. Following World War II, Romania found itself inside the Soviet sphere of influence, with Communist rule officially declared in 1947. In April 1964, when Romania published a general policy paper worked out under Gheorghe Gheorghiu-Dej's instructions, the country was well on its way of carefully breaking away from Soviet control. Nicolae Ceaușescu became the country's leader the following year. Under his rule, Romania experienced a brief waning of internal repression that led to a positive image both at home and in the West. However, repression again intensified by the 1970s, and Ceaușescu's regime eventually became one of the most repressive in the world and one of the most repressive of modern times.
Sources: en.wikipedia.org
musculoskeletal pain neck pain muscle spasms extremity pain muscle fatigue anaphylaxis malignancy The most common adverse effect of reslizumab was oropharyngeal (mouth and throat) pain. According to the phase III clinical trials data, oropharyngeal pain occurred in ≥2% of individuals along with elevated baseline creatine phosphokinase (CPK), which was more common in patients treated with reslizumab versus placebo. Myalgia was also reported more in patients in the reslizumab 3 mg/kg group versus the placebo group as well as some musculoskeletal adverse reactions. Lastly, some serious adverse reactions that occurred in subjects treated with reslizumab but not in those treated with placebo included anaphylaxis and malignancy.
President Donald Trump said that Vance, Witkoff, and former senior presidential adviser Jared Kushner are talking to intermediaries in Pakistan on ending the war. He also called the Iran proposal a "significant step" ahead of his Tuesday deadline for Iran to reopen the Strait of Hormuz. Earlier on 7 April, Trump warned that "a whole civilization will die tonight" and will "never be brought back" if Iran does not agree to a deal by midnight (GMT). Later during the day, amidst a two-week ceasefire plan by Pakistan, White House Press Secretary Karoline Leavitt stated that Trump was made aware of the plan. Additionally, it was reported by CBS News that Vance would serve as the US interlocutor in the ceasefire talks. On 8 April, Trump threatened to impose a 50% tariff on any country 'supplying military weapons to Iran.' Also on 8 April, Trump threatened that if no deal is reached by Wednesday when the ceasefire expires, the fighting may resume. On 21 April, Trump said that Iran has violated the ceasefire "numerous times." At an 8 April press conference, Trump said the US will work closely with Iran, talking about the tariff, sanctions and relief. In regard to the Iranian uranium, he stated: "There will be no enrichment of Uranium, and the United States will, working with Iran, dig up and remove all of the deeply buried (B-2 Bombers) Nuclear 'Dust.'" He later added that Lebanon is not included in the ceasefire agreement and that Hezbollah will need to be dealt with: Yeah, they [Lebanon] were not included in the deal . . Because of Hezbollah. They were not included in the deal.
=== Intravenous administration === Many forms of medication (from antibiotics to chemotherapy) are administered intravenously, as they are not readily or adequately absorbed by the digestive tract. After severe acute blood loss, liquid preparations, generically known as plasma expanders, can be given intravenously, either solutions of salts (NaCl, KCl, CaCl2 etc.) at physiological concentrations, or colloidal solutions, such as dextrans, human serum albumin, or fresh frozen plasma. In these emergency situations, a plasma expander is a more effective life-saving procedure than a blood transfusion, because the metabolism of transfused red blood cells does not restart immediately after a transfusion.
==== Dextromethorphan ==== Dextromethorphan/bupropion, sold under the brand name Auvelity, is a combination medication approved by the US FDA in 2022 for the treatment of major depressive disorder (MDD) in adults. The formulation pairs dextromethorphan, an N-methyl-D-aspartate (NMDA) receptor antagonist and sigma-1 receptor agonist, with bupropion, a norepinephrine-dopamine reuptake inhibitor that also functions as a CYP2D6 enzyme inhibitor. Bupropion is included in the combination to slow the metabolism of dextromethorphan by inhibiting CYP2D6, thereby increasing its bioavailability and allowing dextromethorphan's potential antidepressant effects to be achieved. While the precise mechanism of action in treating depression is not fully understood, it is hypothesized that the medication works by modulating glutamate signaling and influencing other neurotransmitter systems.
=== Limitations === The minimization of radiation dose to the subject is an attractive feature of the use of short-lived radionuclides. Besides its established role as a diagnostic technique, PET has an expanding role as a method to assess the response to therapy, in particular, cancer therapy, where the risk to the patient from lack of knowledge about disease progress is much greater than the risk from the test radiation. Since the tracers are radioactive they are generally not used with those who are pregnant. Limitations to the widespread use of PET arise from the high costs of cyclotrons needed to produce the short-lived radionuclides for PET scanning and the need for specially adapted on-site chemical synthesis apparatus to produce the radiopharmaceuticals after radioisotope preparation. Organic radiotracer molecules that will contain a positron-emitting radioisotope cannot be synthesized first and then the radioisotope prepared within them, because bombardment with a cyclotron to prepare the radioisotope destroys any organic carrier for it. Instead, the isotope must be prepared first, then the chemistry to prepare any organic radiotracer (such as FDG) accomplished very quickly, in the short time before the isotope decays. Few hospitals and universities are capable of maintaining such systems, and most clinical PET is supported by third-party suppliers of radiotracers that can supply many sites simultaneously.
Sources: en.wikipedia.org
两者都是 GHS-R1a 激动剂，但 ipamorelin 在研究中显示出更高的生长激素释放选择性。早期资料显示它对皮质醇、催乳素与食欲的刺激弱于 GHRP-6。这些差异是相对程度，而非绝对区分。
公开资料中它主要以研究用肽的形式出现，未获主要监管机构批准用于治疗。可得材料通常标注仅供研究使用。任何临床用途的宣称都缺少监管依据。
序列中的 Aib 与 D-2-Nal 等非天然残基可提高对肽酶的抵抗能力，并影响受体结合的构象。这类修饰在合成肽设计中较为常见。它们也使常规氨基酸分析需要额外步骤才能确认序列。
Aib 即 α-氨基异丁酸，是一种非蛋白质源氨基酸，其侧链为两个甲基。它在肽链中倾向于诱导螺旋构象并限制骨架的柔性。这种刚性被认为有助于抵抗蛋白酶切割。