GHS-R1a raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.
This page was last updated on 2025-10-31 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。
Ipamorelin is a synthetic pentapeptide that belongs to the growth hormone secretagogue class. It acts as an agonist at the ghrelin receptor, also called the growth hormone secretagogue receptor type 1a. The compound was designed in the 1990s during a search for agents that release growth hormone with fewer off-target hormonal effects than earlier secretagogues. It appears in the research literature under several sequence-based names. Material supplied for laboratory work is normally a lyophilized solid, and it is not marketed as an approved therapeutic in major jurisdictions.
The molecule contains five residues, including alpha-aminoisobutyric acid, D-2-naphthylalanine, and D-phenylalanine, and it ends in a lysine amide. Non-natural and D-configured residues make the chain less susceptible to common peptidases, which helps explain its resistance to rapid breakdown. Its molecular formula is C38H49N9O5, corresponding to a free-base mass near 711.9 daltons. The C-terminal amide removes a negative charge and is a recurring feature in receptor-active peptides of this family. These structural choices are usually discussed as the basis for its selectivity profile.
| 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 |
Compared with earlier growth hormone secretagogues such as GHRP-6 and hexarelin, ipamorelin has been reported to produce less stimulation of adrenocorticotropic hormone, cortisol, and prolactin in animal and early human studies. This selectivity is usually attributed to differences in receptor subtype interactions and to the tissue distribution of the receptor. Effects on appetite appear weaker than those of ghrelin itself, although the supporting evidence base is small. Whether these differences produce a distinct clinical profile remains an open question, since controlled human trials are limited.
Ipamorelin is a synthetic pentapeptide first described in the 1990s by researchers at Novo Nordisk during a program to develop selective growth hormone secretagogues. Its sequence is Aib-His-D-2-Nal-D-Phe-Lys-NH2, incorporating two non-natural residues, alpha-aminoisobutyric acid and D-2-naphthylalanine. The C-terminus is amidated, and the material is supplied as a white lyophilized powder. The molecular formula is C38H49N9O5 and the monoisotopic mass is approximately 711.85 daltons. The short chain and modified residues give it greater resistance to enzymatic degradation than many larger peptide hormones.
At the molecular level, ipamorelin acts as an agonist at the growth hormone secretagogue receptor type 1a, the same G protein-coupled receptor that binds ghrelin. Receptor activation couples to Gq/11 signaling, raising intracellular calcium through inositol trisphosphate and diacylglycerol, which in turn promotes exocytosis of growth hormone from pituitary somatotroph cells. Ipamorelin binds this receptor with high affinity and shows weak activity at other secretagogue-related targets in vitro. Its action requires the intact receptor and is not reversed by growth hormone-releasing hormone antagonists.
Storage recommendations for ipamorelin usually focus on temperature, moisture, and light. Lyophilized powder is typically held at or below minus twenty degrees Celsius in a desiccated container protected from light. Reconstituted solutions are often aliquoted and stored at minus eighty degrees Celsius to reduce repeated freeze-thaw cycles, which can promote aggregation or degradation. The optimal buffer and pH depend on the specific assay, and no single condition applies to every experimental context. Peptide stability should be assessed with time-point measurements rather than assumed from general handling rules.
In the scientific literature, ipamorelin appears mainly in preclinical studies, receptor binding assays, and reviews of growth hormone secretagogues. Authors often discuss its selectivity profile alongside limitations such as small sample sizes, short study durations, and differences between species. Some papers examine pharmacokinetics and clearance, but human data are limited and not sufficient to define general clinical effects. Regulatory discussion treats the compound as an investigational or research substance rather than an approved therapy in most jurisdictions. Open questions include oral bioavailability, long-term endocrine effects, and whether selectivity observed in animals persists in humans.
Ipamorelin is a synthetic pentapeptide that belongs to the growth hormone secretagogue family. Its sequence is Aib-His-D-2-Nal-D-Phe-Lys-NH2, and its molecular mass is approximately 711.9 daltons. The compound was described in the late 1990s by researchers seeking molecules that release growth hormone with fewer side effects than earlier secretagogues. It is a laboratory and research compound, not an approved medicine in most jurisdictions.
At the molecular level, ipamorelin acts as an agonist at the growth hormone secretagogue receptor, also called the ghrelin receptor or GHS-R1a. Binding to this receptor on pituitary somatotroph cells triggers a signaling cascade that leads to growth hormone release. The effect is mediated through phospholipase C and calcium mobilization rather than through the cyclic AMP pathway used by growth hormone releasing hormone. The two pathways are complementary, and combined stimulation produces a larger response than either alone.
=== The Human Metabolome Database === The Human Metabolome Database (HMDB) is a freely available, open-access database containing detailed data on more than 40,000 metabolites that have already been identified or are likely to be found in the human body. The HMDB contains three kinds of information:
==== Variable phenomena – dependently arisen processes ==== The principle of conditionality, which is real and stable, is contrasted with the "dependently arisen processes", which are described as "impermanent, conditioned, dependently arisen, of a nature to be destroyed, of a nature to vanish, of a nature to fade away, of a nature to cease." SA 296 describes them simply as "arising thus according to causal condition, these are called dharmas arisen by causal condition."
=== Seizures === Levetiracetam is an anti-epileptic drug than can be used to treat partial and generalized seizures. Levetiracetam inhibits P/Q channel-mediated glutamate release and decreases the excitatory post synaptic currents of both AMPA and NMDA receptors in the hippocampus, specifically the dentate gyrus, which is known to propagate seizure activities. The inhibition of glutamate release results in an anti-epileptic response in patients because it decreases the excitatory postsynaptic current. There are many different types of calcium channels, so to prove that the P/Q type calcium channels are directly involved, a P/Q type voltage gated calcium channel inhibitor, omega-agatoxin TK, was used to block the channel. When blocked, patients no longer benefited from the anti-epileptic effects from the drugs. When blockers for L type and N type calcium channels were used, the effects of Levetiracetam were still seen. This is strong evidence that the P/Q type calcium channels are involved in the Levetiracetam treatment which allow for relief from seizures.
=== Bacterial or viral === As bacterial and viral infections can both cause the same kinds of symptoms, it can be difficult to distinguish which is the cause of a specific infection. Distinguishing the two is important, since viral infections cannot be cured by antibiotics whereas bacterial infections can.
Sources: en.wikipedia.org
== Cyber counterintelligence == Cyber counter-intelligence are measures to identify, penetrate, or neutralize foreign operations that use cyber means as the primary tradecraft methodology, as well as foreign intelligence service collection efforts that use traditional methods to gauge cyber capabilities and intentions.
=== Cryopulverization === Samples with a tough extracellular matrix, such as animal connective tissue, some tumor biopsy samples, venous tissue, cartilage, seeds, etc., are reduced to a fine powder by impact pulverization at liquid nitrogen temperatures. This technique, known as cryopulverization, is based on the fact that biological samples containing a significant fraction of water become brittle at extremely cold temperatures. This technique was first described by Smucker and Pfister in 1975, who referred to the technique as cryo-impacting. The authors demonstrated cells are effectively broken by this method, confirming by phase and electron microscopy that breakage planes cross cell walls and cytoplasmic membranes. The technique can be done by using a mortar and pestle cooled to liquid nitrogen temperatures, but use of this classic apparatus is laborious and sample loss is often a concern. Specialised stainless steel pulverizers generically known as Tissue Pulverizers are also available for this purpose. They require less manual effort, give good sample recovery and are easy to clean between samples. Advantages of this technique are higher yields of proteins and nucleic acids from small, hard tissue samples - especially when used as a preliminary step to mechanical or chemical/solvent cell disruption methods mentioned above.
=== Appearance and form === DMT is commonly handled and stored as a hemifumarate, as other DMT acid salts are extremely hygroscopic and will not readily crystallize. Its freebase form, although less stable than DMT hemifumarate, is favored by recreational users choosing to vaporize the chemical as it has a lower boiling point. DMT is a lipophilic compound, with an experimental log P of 2.57.
=== 2000 === 13 March The Secret Life of the Crash Test Dummy, about the biomechanics of car crashes; a typical crash test dummy cost around £100,000, with about three hundred individual parts, that had to be included by safety law, and new cars could not be sold until the dummy had tested it sufficiently; the Volvo 300 1980s television advert; Lt-Col Wayne Mattson of the USAF and a strange crash in New Mexico, one hundred miles north of the Trinity (nuclear test), and near White Sands Missile Range, where German V-2 missiles were being tested, which were conveniently blamed by the USAF on anthropomorphic dummies; John Melvin (engineer) and the legacy of USAF biophysicist and doctor Colonel John Stapp, who mostly invented aviation safety testing; John Stapp conducted gruesome horrific deceleration tests on himself; Alderson had made artificial limbs for injured USAF World War II pilots, so made a full artificial proto-human; John Stapp tested his dummies in vehicles; Clarence Ditlow and the Center for Auto Safety; in 1966 it became legal in the US for new cars to have been tested by dummies; mathematical models of injury were needed, to translate the acquired crash data into possible effects on the human body, worked out by mechanical engineer Walter Pilkey of the University of Virginia; Scottish orthopaedic surgeon Angus Wallace and impact speed on bone tensile strength; in 1976 the Hybrid III dummy was designed, the automotive industry standard design; David Abbott, advertising executive; the data for designing the crash test dummy, Hybrid III, was mostly derived from data procured for human male occupants - and typical (fiftieth percentile) males, not female, and females had much different bodies; child dummies were essentially smaller adult male dummies, which was not biologically true; new dummies were developed at the National Transportation Biomechanics Research Center. Narrated by Andrew Lincoln, produced by Cathy Rogers, directed by Peter Webber, made by RDF Television. Shown on Wednesday 17 January 2001 on The Nature of Things in Canada 20 March Rise and Fall of GM Food, about genetically modified food; Belgian geneticist Marc Van Montagu, of the University of Ghent, visits Havana in Cuba, where a new research centre opened with Carlos Borroto; protests by topless women; GM was largely first developed by Mexican geneticist Herrera Estrella, of the Centre of Investigation and Advanced Studies; Rob Fraley of Monsanto; US farmers spend $8bn dollars on herbicides and pesticides; Roger N. Beachy had a breakthrough in 1986 at the Washington University in St. Louis, now at the Donald Danforth Plant and Science Center; Monsanto made the first insecticide-resistant plant in 1987; many African farmers cannot afford insecticides; Cyrus Ndiritu of the Kenya Agriculture Research Institute; much food harvested in Africa does not last before it reaches the consumer; in 1990 Don Grierson of the Plant Science Division of the University of Nottingham found genes of ripening; Channapatna Prakash of Tuskegee University in Alabama; aluminium toxicity of soils in tropical countries affected yield; Julian Borger of The Guardian; biologist Mae-Wan Ho of the Open University; biologist John Gatehouse of the University of Durham, and the Pusztai affair at The Rowett Institute; Helen Browning, Chairman of the Soil Association; former Vice-Chancellor of UEA, Derek Burke; former Independent environment correspondent Richard D. North, who had grown out of love with the hard-line environmental movement; European farmers grew five times more produce than they did in the 1960s, and there were twice as many trees in the UK than in the 1920s; Renée Elliott of Planet Organic; around 100m children in Third World countries suffered from Vitamin A deficiency. Directed by Martin Durkin, made by his company Kugelblitz 27 March Simply Complex, about the physicist Murray Gell-Mann; by an accident, he devised strangeness of sub-atomic particles, in his mid-20s; he predicts an omega minus particle, which was found in 1962; he predicts that the proton and neutron were made of three triplet particles, which he called quarks from Finnegans Wake and his Eightfold way (physics), also predicted by George Zweig; he worked closely with Richard Feynman at Caltech in the 1960s; on 30 October 1969 he is told that he had won the Nobel Prize for Physics; his friendship with MIT mechanical engineer Seth Lloyd; British physicist Geoffrey West; the documentary is in a biographic informal style that Horizon has since often followed. Produced by Barbara Altounyan, directed by Celia Lowenstein, made by Diverse Productions 3 April Meningitis - Search for a Cure, 3,000 people in the UK had meningitis in 1999; microbiologist Martin C. J. Maiden; one in five died from meningococcal disease; damage is caused by the endotoxin (lipopolysaccharide); a healthy survey is carried out at Burford School; Mike Levin (paediatrician) at Imperial College, and how meningitis A is a huge danger in Africa; 60% of cases in the UK are meningitis B, and many such cases are treated at St Mary's Hospital, London; Brett Giroir of the Children's Medical Center Dallas; 17-year-old Amy Mansell from Whitstable was in a coma for five weeks. Narrated by Paul Brightwell, produced by David Dugan, directed by Jeremy Llewellyn-Jones, made by Windfall Films with Nova and WGBH Boston. It was shown on Nova as Killer Disease on Campus, episode 9 of season 29, shown on 3 September 2002, and shown under the original programme title as a half-hour programme on 6 November 2003 on Catalyst on ABC in Australia 10 April The Box, about flight recorders, with ValuJet Airlines Flight 592 which crashed on 11 May 1996; voice recorders have been compulsory since the late 1960s; Dukane Seacom make emergency underwater locator beacons (ULBs); the Boeing 737, which had around 21,000 take-offs per day, was believed to have unreliable rudder control since the 1980s, as shown in the United Airlines Flight 585 crash on 3 March 1991, having had two rudder incidents in the previous two weeks, with the aircraft flipping 35 seconds after take-off and crashing all in seven seconds; the electrohydraulic servo valve in the Boeing 737 rudder control unit was thought to be sometimes temperamental; Boeing claimed that the March 1991 crash was due to a rotor or lee wave, caused by nearby mountains; the USAir Flight 427 crash on 8 September 1994, where the aircraft flipped at 6,000 ft, in 28 seconds crashing; British Airways did not rely on their Penny & Giles quick access recorders, and would consolidate this data where anomalies were checked, so the NTSB needed BA's data for their 737 aircraft; this safer BA method was introduced by the previous British European Airways (BEA) when it had to prove to the CAA that its autoland system for the Trident was safe, in the Civil Aircraft Airworthiness Data Recording Programme which since 1990 has been collected by the British Airways Safety Information System (BASIS); the 1991 crash investigation concluded after 8 years in 1999, with Boeing ordered to redesign the servo valve. 9 October Full Throttle, about the technology and psychology of motor racing; Brazilian driver Christian Fittipaldi; the Eurofighter, controlled by computers, and due to enter RAF service in 2002; Archie Neill, BAE test pilot; Stephen Olvey, motor racing medical officer; driver Mark Blundell; the Long Beach Grand Prix in Los Angeles; Steve Clark, engineer for Mercedes; Brian Lisles and Peter Gibbons of Newman Haas Racing; the edge of performance envelope; Mario Andretti, former driver: Edward Winter of Sheffield Hallam University and predicting outcomes in sport, by intuition; John Rothwell of the Institute of Neurology in London, testing reflexes, by an MRI scanner, and how the brain stores instructions; psychologist Mike Land of the University of Sussex, and the psychology of prediction, and feedforward; life expectancy of racing drivers in the 1970s was short; racing drivers had risk positive personalities, and became accustomed to risk; psychologist Tim Wheeler; Jimmy Vasser of Chip Ganassi Racing; a female violinist plays La fille aux cheveux de lin; sports psychologist Brian Hemmings; Austrian driver Alexander Wurz of Benetton Formula; RAF SEPECAT Jaguar XZ103 of 41 Squadron; engineer Pat Symonds of Benetton Racing; Simon Taylor (journalist) of Motor Sport; Graham Rood of DERA Air Systems in north Hampshire. Narrated by Stephen Rashbrook, produced by Patrick Uden, directed by Andy Robbins, made by Uden Associates 16 October Lethal Seas: the Maelstrom, about ocean whirlpools; the Gulf of Corryvreckan in Scotland, Lofoten and Saltstraumen in Norway; with Prof Tsukasa Nishimura of Tokyo University of Science and Prof Walter Munk of the Scripps Institution of Oceanography; the Firth of Lorn in west Scotland has one of the world's most dangerous whirlpools, the Royal Navy avoids it; atmospheric physicist Peter Read; mathematician David Dritschel, and the Great Red Spot vortice; the dangerous Arran Rapids on the Cordero Channel in western Canada; Burkard Baschek of the Institute of Ocean Sciences, who dropped a CTD (instrument) into the torrential river currents; Tremble Island in the notorious Slingsby Channel, where a geophone was placed; the novel A Descent into the Maelström; Bjørn Gjevik, a fluid dynamicist in the Department of Mathematics, at the University of Oslo; strong tidal currents in the Naruto Strait in Japan, and the Naruto whirlpools. Narrated by Stephen Rashbrook, produced by Robert Sproul-Cran, directed by Kim Flitcroft, made by Northlight Productions with the Discovery Channel 23 October Einstein's Biggest Blunder, about calculations of the expansion of the universe; the documentary opens with a pastiche of the Star Wars opening credits; two physicists met in 1996, with a new radical proposal for explaining the many anomalies in the expansion of the universe - Andreas Albrecht (cosmologist) of the University of California, Davis and João Magueijo of Portugal; Dave Wark of the University of Sussex, visits Bern in Switzerland; Ruth Durrer of the University of Geneva; John E. Baldwin of the University of Cambridge, and the 1887 Michelson–Morley experiment, which found that the Earth's rotational speed did not affect the speed of light in any way, alongside the Venus movement of The Planets; to account for this, Einstein made his field equations, and lambda - the cosmological constant was added by Einstein to account for how space-time would need to expand; Einstein's equations inferred that the expansion of the universe rested on inherently unstable conditions; due to the Doppler effect, background radiation from the Big Bang is now perceived as microwave radiation; Richard Ellis (astronomer) of Caltech; Einstein didn't believe in the Big Bang until a meeting with Hubble in 1932 in California; with the new theory of an expanding universe, the cosmological constant was now required, but the precise trajectory of the expansion of the universe could not be directly predicted, which led to the flatness problem; the theory of inflation was put forward by Alan Guth in the 1970s; when at St John's College, Cambridge, João Magueijo had the radical proposal that if the speed of light was higher, in the early universe, a cosmological horizon of sufficient distance would be possible, to explain the predicted conditions of the expansion of the early universe, and the cosmological constant problem; the Royal Society gave him a research fellowship to work at Imperial College; as further exploratory work was clocked up, with calculations inclya variable speed of light, the team of physicists looked at other applications for their controversial proposals, such as the flatness problem, and what happened before the Big Bang; in 1998 astrophysicist John Webb, at the University of Cambridge, worked on the theory of a variable speed of light, through investigating quasars, the most distant objects that can be seen; and by looking at supernovae, it was largely expected that any recorded data would show indications of a deceleration in the rate of expansion of the universe, but the data instead showed that the rate of expansion was - increasing, which led to the lambda-CDM model. Narrated by Scottish actor Matthew Zajac, directed by David Sington, made by Dox Productions 30 October The Science of Stress, with 42-year-old actor Angus Kennedy; endocrinologist Stafford Lightman of the University of Bristol; Vivette Glover, a perinatal psychobiological at Imperial College; Sir Cary Cooper, psychologist at the former UMIST; Carolyn M. Mazure, psychiatrist at Yale School of Medicine; Charles Nemeroff, psychiatrist at Emory University School of Medicine. Narrated by Geoffrey Palmer, directed by Michael Samuels, produced by Bridget Sneyd, made by Lion Television and the Discovery Health Channel 7 December Science of Crime - Psychopath, with psychologists Robert D. Hare and Adrian Raine, about the psychopathic traits of insincere superficial charm, on the Psychopathy Checklist. Narrated by Neil Pearson, directed by John Purdie, produced by Rosalind Arden, made by Union Pictures 14 December Science of Crime - Criminal Evidence, about the forensic psychologist 49-year-old Kathy Reichs. Produced by Geoff Deehan, directed by Roger Pyke, made by Yap Films 21 December Science of Crime - Cybercops, the Hackers on Planet Earth conference; Cult of the Dead Cow, founded by Swamp Rat, and its Back Orifice software for accessing Windows 98; the Happy99 virus; wardialing; part of the High Technology Theft Apprehension and Prosecution Program in California. Narrated by Steven Mackintosh, written by Callum Macrae, directed by Witold Starecki
== Toxicity == The Pompilidae family of spider wasps is known for its powerful and painful sting that is used to paralyse arachnids. Social wasps readily attack any threat to their queen and colony and are the only type of insects responsible for medically significant incidents with humans. However, PMTXs are produced by solitary spider wasps and since solitary wasps do not have a colony to defend, humans normally will not be stung by these wasps. PMTX is not listed by IARC, which suggests that there is no indication of carcinogenicity for humans, other information about the effects of PMTX on humans is currently not available. However, it is thought that it won't have a big impact on humans due to the difference in neurological setup between humans and arachnids. What is known is that being stung by a spider wasp causes local pain and swelling, and some people might have an allergic reaction to the sting which can be dangerous. The symptoms of a spider wasp sting, apart from the allergic reaction, can be treated with a cold compress. Even though humans usually will not be stung by these wasps, there have been scientists that deliberately extensively provoked spider wasps similar to PMTX-producing spider wasps, to have them stung by these animals for research on the pain inflicted by these insects. Because of these individuals, it is known that though spider wasp venom causes paralysis in their arthropod prey, they inflict intense pain that remains for around five minutes onto vertebrates such as humans.
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。