A practical reference on intranasal delivery: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2025-09-14. Anything still debated is marked as such rather than presented as settled.
常规纯度与身份确认依赖反相高效液相色谱,并辅以质谱测定分子量。氨基酸组成分析可用于验证序列构成,肽图分析则能进一步定位修饰或降解产物。杂质谱通常关注缺失序列肽、截短片段和氧化产物。不同方法的检出限并不相同,因此各实验室报告的纯度数值不宜直接横向比较。
多数实验室与市售的 Semax 以冻干粉形式提供。冻干粉通常建议保存在 -20 °C 或更低温度下,同时避免光照与反复升温。短期运输有时采用冷藏条件,但长期保存仍以冷冻为主。分包操作应尽量减少开盖次数,以降低吸湿和微生物污染的风险。开封后若未一次用完,建议在干燥环境中密封并尽快放回低温储存。
溶液状态的稳定性明显低于冻干粉。肽类在水溶液中可能经历水解、氧化与聚集,其中甲硫氨酸和天冬酰胺等残基常是敏感位点。Semax 含有甲硫氨酸,因此氧化风险相对突出。工作液一般主张现配现用,或冷藏并在数日内用尽。缓冲液种类、pH 和离子强度都会影响降解速率,而关于最佳条件的公开数据并不统一。
The proposed mechanism centres on neurotrophic signalling rather than direct receptor activation. Semax is reported to increase expression of brain-derived neurotrophic factor and nerve growth factor in several brain regions, and to shift the balance between excitatory and inhibitory neurotransmitter systems. Interaction with melanocortin receptors has been suggested because of the parent ACTH fragment. Many of these findings come from rodent studies, and the extent to which they translate to human physiology remains an open question.
Scientific literature on semax is unevenly distributed. A substantial share of published work originates from a small number of laboratories in Russia, while independent replication elsewhere is limited. Human data consist mostly of small trials with short follow-up, and several reported outcomes rely on subjective rating scales. Questions about how much intact peptide reaches the central nervous system after nasal administration, and how long it persists there, are still unresolved. The compound is best described as an active research subject rather than a settled pharmacological agent.
Semax is a synthetic heptapeptide with the sequence Met-Glu-His-Phe-Pro-Gly-Pro. It was derived from the ACTH(4-10) fragment, a short segment of adrenocorticotropic hormone that lacks the hormonal activity associated with the full-length peptide. Researchers at the Institute of Molecular Genetics in Moscow developed the compound during the 1980s. It has been registered as a pharmaceutical product in Russia and several neighbouring countries, where it is supplied as a nasal solution, and it is also sold internationally as a research chemical.
| Property | Value | Notes |
|---|---|---|
| 外观 | 白色至类白色粉末 | 常见于冻干制剂 |
| 溶解度 | 易溶于水 | 在极性溶剂中一般也可溶 |
| 建议储存温度 | -20 °C | 冻干粉,避光密封 |
| 常见分析手段 | 反相高效液相色谱 | 常与质谱联用 |
| 主要降解路径 | 水解与氧化 | 溶液状态更显著 |
Identity and purity of semax are established with reversed-phase high-performance liquid chromatography coupled to ultraviolet detection, usually at 214 nanometres. Mass spectrometry, most often electrospray ionisation in positive mode, confirms the molecular mass and reveals truncated sequences. Amino acid analysis and peptide mapping after enzymatic digestion provide additional structural confirmation. Laboratories typically report purity as the percentage area of the main peak, a figure that does not capture isomeric or oxidised variants unless the method resolves them.
The peptide is prone to several degradation pathways. Oxidation of the methionine residue produces a sulfoxide that elutes close to the parent peak in many chromatographic systems. Hydrolysis of peptide bonds and deamidation of susceptible residues in related sequences also reduce purity over time. Lyophilised material kept dry at minus twenty degrees Celsius and shielded from light is the most stable form commonly described in laboratory practice.
Laboratory descriptions of the material are consistent across suppliers. It appears as a white to off-white lyophilized powder that dissolves readily in water and in polar organic solvents such as dimethyl sulfoxide. Aqueous solutions are clear and colorless at low concentrations. Because the peptide contains methionine, oxidation at the sulfur atom is a recognized degradation pathway, and handling notes usually call for protected, desiccated storage. Reported purity for research-grade lots is generally above 95 percent as measured by reversed-phase high-performance liquid chromatography.
The compound is registered in Russia as a pharmaceutical product, most commonly formulated as a nasal solution, and has been used in that setting since the 1990s. Outside that jurisdiction it is generally handled as a research chemical rather than an approved medicine. Regulatory status therefore differs sharply between countries, and material sold internationally may not correspond to the Russian pharmaceutical formulation. Documentation with commercial samples is typically limited to a certificate of analysis covering purity and identity, not clinical status or local legal classification.
Semax is a synthetic heptapeptide with the sequence Met-Glu-His-Phe-Pro-Gly-Pro. It corresponds to the ACTH(4-7) fragment extended at the C-terminus by a Pro-Gly-Pro tripeptide, an addition intended to slow enzymatic breakdown. The molecular formula is C37H51N9O10S and the molecular mass is approximately 814 daltons. In the literature it is often described as an ACTH(4-10) analog, although that label reflects a naming convention as much as a precise structural relationship. The compound was developed in Russia and remains most closely associated with that research tradition.
Pharmacokinetic accounts emphasize rapid breakdown. After intravenous dosing the intact peptide disappears from blood within minutes, and nasal delivery produces low but measurable concentrations. Metabolites rather than the parent molecule may account for part of the observed activity, although the relative contribution is unresolved. Dosing in the literature varies widely and no optimal schedule has been agreed. These gaps are regularly cited as a reason the findings have not produced broad clinical adoption beyond the original research setting.
Proposed mechanisms center on neurotrophic signaling rather than on classical melanocortin receptor activation. Rodent experiments have reported shifts in the expression of brain-derived neurotrophic factor and nerve growth factor after administration, together with changes in the associated receptor systems. Several authors argue that the peptide acts largely through its degradation products and their interaction with peptidergic pathways, but this remains a hypothesis rather than a settled finding. No single molecular target has been identified in a way that the field broadly accepts.
Published research covers ischemic stroke, traumatic brain injury, cognitive impairment, optic nerve conditions and attention-related measures. Much of the human evidence comes from small trials conducted in one country, which limits how far the results generalize. Animal models supply the larger share of the data, and effects seen in rodents do not transfer automatically to people. Reviews have noted that methodological reporting is often incomplete, making it difficult to pool results or compare treatment schedules across studies.
当时的短肽研究普遍关注能否穿越血脑屏障、在低剂量下产生中枢效应,Semax 属于这一路线。鼻内给药是其主要使用方式,俄语文献报道的适应症涵盖缺血性卒中、短暂性脑缺血发作、认知功能减退以及视神经病变。这些研究大多发表在当地期刊上,样本规模与终点设置同西方试验惯例存在差异,国际同行对其临床证据的强度看法不一。
各国监管态度分化明显。俄罗斯按处方药管理,部分东欧国家留有使用记录;欧盟与美国未批准其作为药物上市,市面流通品通常标注为研究用化学品。身份差异意味着标示含量、纯度与无菌性缺少统一核查。体育领域还牵涉反兴奋剂名录,跨境携带则受目的地药品法规约束。
Partial agonism and signaling bias describe distinct pharmacological properties: partial agonism refers to the maximum response produced relative to a reference full agonist, whereas signaling bias describes the relative preference for different intracellular signaling pathways activated by the same receptor. Activation of MOR primarily couples the receptor to inhibitory Gi/o proteins, resulting in inhibition of adenylyl cyclase, reduced intracellular cyclic AMP (cAMP), modulation of potassium and calcium channels, and decreased neuronal excitability and neurotransmitter release. β-Arrestin recruitment represents a partially distinct signaling and regulatory pathway involved in receptor desensitization, trafficking, and internalization. Consequently, a ligand may display partial efficacy for G-protein signaling while producing substantially weaker β-arrestin recruitment. MORs may also form receptor homomers containing more than one receptor protomer. Therefor occupancy of one protomer by a partial agonist does not necessarily prevent a second ligand from occupying the other orthosteric binding site of the second protomer. Thus, a 48%-efficacy partial agonist and a second partial agonist exhibiting 66% efficacy would occupy the second separate protomer within the same receptor complex. Buprenorphine was patented in 1965, FDA approved for medical use as an analgesic in 1981, and FDA approved for treating opioid use disorder in 2002. It is on the World Health Organization's List of Essential Medicines.
=== Approval === It is approved to treat complicated skin and soft tissue infections (cSSTI), complicated intra-abdominal infections (cIAI), and community-acquired bacterial pneumonia (CAP) in individuals 18 years and older. In the United Kingdom it is approved in adults and in children from the age of eight years for the treatment of complicated skin and soft tissue infections (excluding diabetic foot infections) and complicated intra-abdominal infections in situations where other alternative antibiotics are not suitable.
The game's plot twist, where the player discovers that the player-character Jack has been coerced into events by the trigger phrase, "Would you kindly...", is considered one of the strongest narrative elements of video games to that point. In homage to BioShock, Black Mirror's video game-centric episode "Playtest" includes the phrase. A sequel, BioShock 2, was announced in 2008, with its development led by 2K Marin. BioShock 2 was released for Windows PC, Mac, Xbox 360, and the PlayStation 3 worldwide on February 9, 2010. Irrational Games developed BioShock Infinite, taking place aboard the collapsing air-city of Columbia in the year 1912. Infinite involves the possibilities of multiple universes. In one scene, the game take place at the lighthouse and bathysphere terminus of Rapture as part of this exploration. However, no direct canonical connection is given in the main game. The episodic expansion, Burial at Sea, takes place in Rapture in 1959, before the war between Atlas and Ryan, while continuing the story of Booker and Elizabeth. This content links the two stories while providing expansion on the causes and behind-the-scenes events alluded to by the in-game background from BioShock. After completing BioShock Infinite and its expansion, Levine announced that he was restructuring Irrational Games to focus on smaller, narrative-driven titles. 2K Games continues to hold on to the BioShock intellectual property and plans to continue to develop games in this series.
It also saw the first "Era of Progress" as the college transformed from a college supported by the religious community (which focused primarily upon training young men and women for the ministry) to a college gaining support from private foundations, and offering liberal arts academic degree for a variety of professions. In 1915, Andrew Carnegie donated to the school a grant of $50,000 for a central academic building. The terms of the grant included the purchase of a new site for the College, payment of all outstanding obligations, and the construction of a building to be named after him. The College met the conditions and moved to its present site in northeast Baltimore in 1917. In 1918, the white community of Lauraville tried to have the sale revoked by filing suit in the circuit court in Towson, upset that the Ivy Mill property, the planned location of Morgan State, had been sold to a "negro" college. The circuit court dismissed the suit, which the community appealed to the Maryland Court of Appeals. The appellate court upheld the lower court decision, finding no basis that siting the college at this location would constitute a public nuisance. Despite some ugly threats and several demonstrations against the project, Morgan College was constructed at the new site and later expanded. Carnegie Hall, the oldest original building on the present Morgan campus, was erected a year later. Morgan remained a private institution until 1939. That year, the state of Maryland purchased the school. Morgan College became Morgan State College.
Sources: en.wikipedia.org
=== Postmortem and forensic === After death, the vitreous resists putrefaction longer than other body fluids. Within the hours, days and weeks after death, the vitreous potassium concentration rises, at such a predictable speed that vitreous potassium levels are frequently used to estimate the time since death (post-mortem interval) of a corpse. The metabolic exchange and equilibration between systemic circulation and vitreous humour is so slow that vitreous humour is sometimes the fluid of choice for postmortem analysis of glucose levels or substances which would be more rapidly diffused, degraded, excreted or metabolized from general circulation. According to Judaism, extracting the vitreous fluid for forensic chemical analysis is preferred to blood analysis (in case a forensic or post-mortem toxicology test is deemed necessary). This avoids the loss of even a few droplets of blood from the body prior to burial.
In 1930 Cecil George Paine, a pathologist at the Royal Infirmary in Sheffield, successfully treated ophthalmia neonatorum, a gonococcal infection in infants, with penicillin (fungal extract) on 25 November 1930. In 1940 the Australian scientist Howard Florey (later Baron Florey) and a team of researchers (Ernst Chain, Edward Abraham, Arthur Duncan Gardner, Norman Heatley, Margaret Jennings, Jean Orr-Ewing and Arthur Gordon Sanders) at the Sir William Dunn School of Pathology of the University of Oxford made progress in making concentrated penicillin from fungal culture broth that showed both in vitro and in vivo bactericidal action. In 1941 they treated a policeman, Albert Alexander, with a severe face infection; his condition improved, but then supplies of penicillin ran out and he died. Subsequently, several other patients were treated successfully. In December 1942, survivors of the Cocoanut Grove fire in Boston, United States, were the first burn patients to be successfully treated with penicillin. The first successful use of pure penicillin was in 1942 when Fleming cured Harry Lambert of an infection of the nervous system (streptococcal meningitis) which would otherwise have been fatal. By that time the Oxford team could produce only a small amount. Florey willingly gave the only available sample to Fleming. Lambert showed improvement from the very next day of the treatment, and was completely cured within a week. Fleming published his clinical trial in The Lancet in 1943.
Technetium 99mTc albumin aggregated (99mTc-MAA) is an injectable radiopharmaceutical used in nuclear medicine. It consists of a sterile aqueous suspension of Technetium-99m (99mTc) labeled to human albumin aggregate particles. It is commonly used for lung perfusion scanning. It is also less commonly used to visualise a peritoneovenous shunt and for isotope venography.
Sources: en.wikipedia.org
一般不建议常温长期保存。多数说明指向 -20 °C 冷冻避光。常温运输通常被视为短期可接受,但会加快降解风险。
公开资料对此没有统一答案。普遍建议现配现用,或冷藏并在数日内用完。含甲硫氨酸的序列更易氧化,放置时间越长风险越高。
反相高效液相色谱是最常用的手段,配合质谱确认分子量。氨基酸组成分析和肽图分析可补充序列层面的验证。
Semax is based on the ACTH(4-10) fragment, a seven-amino-acid segment of adrenocorticotropic hormone. The synthetic peptide retains the core sequence while removing regions associated with endocrine activity. This modification is intended to isolate effects on the nervous system.