intranasal delivery is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.
Updated 2026-04-28. Numbers and descriptions here follow the published literature rather than marketing material.
Regulatory status varies sharply by country. Semax is registered for medical use in Russia, where it appears in formularies as a nasal solution, and it also holds registration in a small number of neighbouring states. It has no approval from the United States Food and Drug Administration or the European Medicines Agency, and it is not a scheduled controlled substance in most jurisdictions. Elsewhere it circulates mainly as laboratory material, so purity documentation comes from suppliers rather than from a national pharmacopoeia.
Semax is a synthetic peptide created in the Soviet Union during the early 1980s by researchers working in Moscow. It was built from the short adrenocorticotropic hormone fragment known as ACTH(4-10), and the chain was then extended with three additional amino acids. The resulting molecule was named semax and entered clinical use in Russia in 1994. It is generally described as a nootropic and neuroprotective agent rather than as a hormone analogue.
The parent fragment ACTH(4-10) carries the sequence Met-Glu-His-Phe-Arg-Trp-Gly. Semax replaces the arginine and tryptophan positions with a proline-glycine-proline tail, giving Met-Glu-His-Phe-Pro-Gly-Pro. That change removes residues associated with adrenal stimulation, so the peptide does not drive cortisol release the way full ACTH does. This distinction shapes how the compound is grouped in the literature, where it sits with neuropeptides and peptide neuromodulators rather than with corticosteroids.
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。
| Property | Value | Notes |
|---|---|---|
| Chemical class | Synthetic heptapeptide | Analogue of the ACTH(4-10) fragment |
| Amino acid sequence | Met-Glu-His-Phe-Pro-Gly-Pro | Single-letter form MEHFPGP |
| Molecular formula | C37H51N9O10S | Free peptide, nominal mass near 814 Da |
| First registration | 1994, Russia | Nasal formulation for neurological indications |
| Typical purity grade | 95% or higher by HPLC | Research material; higher grades used as reference standards |
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。
Semax 是人工设计的七肽,序列为 Met-Glu-His-Phe-Pro-Gly-Pro,骨架取自促肾上腺皮质激素片段 ACTH(4-10)。它于二十世纪八十年代在苏联的分子遗传学研究机构内合成。设计目标是保留该片段与注意力和记忆相关的活性,同时剔除促皮质激素释放等内分泌作用。此后俄罗斯将其登记为药品并进入临床使用。
Lyophilized material is chemically stable for extended periods when kept dry, cold, and protected from light. The powder is hygroscopic, so vials should be warmed to room temperature before opening to reduce condensation on the contents. Once dissolved, the peptide is far less stable because peptide bonds are susceptible to hydrolysis and the methionine residue can oxidize. Solutions are typically aliquoted and held at 2-8 °C for short intervals or frozen for longer ones, and repeated freeze-thaw cycles should be avoided.
Routine characterization relies on reversed-phase high-performance liquid chromatography to establish purity and on mass spectrometry to confirm molecular identity. Electrospray ionization and matrix-assisted laser desorption ionization are both used for mass verification. Amino acid analysis and peptide mapping can detect sequence errors. Common impurities include truncated sequences, methionine sulfoxide formed by oxidation, and deamidated products. Chromatograms are usually recorded near 214 nm, where the peptide backbone absorbs, and purity is reported as the percentage area of the principal peak.
The compound was developed during the 1980s at the Institute of Molecular Genetics in Moscow as part of research on fragments of adrenocorticotropic hormone. Early work examined short ACTH-derived sequences that retained neurotrophic effects while lacking the endocrine activity of the full hormone. Semax entered clinical use in Russia during the 1990s, where it received registration for several neurological indications. Outside that region it remained primarily a laboratory research material rather than an approved therapeutic. English-language literature on it grew more slowly and frequently cited the original Russian studies.
Terminology around the compound varies by source. It appears in catalogues and papers as Semax, as the heptapeptide ACTH(4-7)-Pro-Gly-Pro, and under various alphanumeric laboratory codes used by individual suppliers. These names refer to the same sequence but may imply different salt forms, purity grades, or counter-ions. Peptide databases usually list the free base mass, while product descriptions sometimes report acetate or trifluoroacetate salts with a different formula weight. Because naming conventions for research peptides are not standardised across vendors, checking the declared sequence and measured mass is more reliable than relying on a trade name alone.
Semax is a synthetic heptapeptide with the sequence Met-Glu-His-Phe-Pro-Gly-Pro. Its design combines the ACTH(4-7) core fragment with a C-terminal Pro-Gly-Pro extension, a modification intended to improve stability and prolong activity. The molecule is hydrophilic, carries no lipid chains or glycosylation, and has a theoretical mass just over 810 daltons in its free form. All seven residues are proteinogenic amino acids, so no non-natural building blocks appear in the backbone. A free N-terminal methionine and C-terminal proline define the unmodified parent peptide.
The mechanisms attributed to semax are inferred from animal and cell studies rather than traced to one confirmed target. The most frequently cited pathway involves increased expression of brain-derived neurotrophic factor and nerve growth factor in hippocampal and cortical tissue. Some work points to engagement of melanocortin receptors, particularly MC4, which the parent ACTH fragment can activate. Effects on dopaminergic and serotonergic signalling have also been reported. No single account explains all observed results, and the relative weight of each pathway remains unsettled.
Published studies examine a fairly narrow set of endpoints. Rodent experiments commonly measure maze learning, infarct volume after induced ischemia, and tissue levels of neurotrophic factors. Clinical reports from Russian centres describe attention, memory and recovery scores in patients after stroke or transient ischemic attack. Most of those human studies are small and few have been repeated by independent groups. Outcome measures differ between studies, which limits direct comparison.
Circulation time for the peptide is short because peptidases cleave it readily. The Pro-Gly-Pro tail is thought to slow breakdown compared with the bare ACTH fragment, but the gain appears modest. Absorption after intranasal dosing is limited, and only a fraction of a dose is expected to reach the central nervous system. Laboratory concentrations therefore sit well above levels achieved systemically, a gap that complicates translation from bench findings to clinical claims.
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=== Role in neural development === Laminin-111 is a major substrate along which nerve axons will grow, both in vivo and in vitro. For example, it lays down a path that developing retinal ganglion cells follow on their way from the retina to the tectum. It is also often used as a substrate in cell culture experiments. The presence of laminin-111 can influence how the growth cone responds to other cues. For example, growth cones are repelled by netrin when grown on laminin-111 but are attracted to netrin when grown on fibronectin. This effect of laminin-111 probably occurs through a lowering of intracellular cyclic AMP.
glycol Any of a class of aliphatic dihydric alcohols in which the two hydroxy groups are bonded to two different carbon atoms, which are usually but not necessarily adjacent to each other; e.g. ethylene glycol (HOCH2CH2OH).
The structures are identified in genetically modified mice and postmortem human brain tissue, sometimes forming independently of amyloid beta plaques, and may represent a potential new therapeutic target.
== Acquisitions == In February 2006, ASCP acquired the cytology product line of the Midwest Institute for Medical Education (MIME). At the time, it was the only national cytology proficiency testing provider. In 2009, ASCP acquired the medical technologist led National Credentialing Agency for Laboratory Personnel (NCA). The baccalaureate-level certification designations Medical Technologist (MT) and Clinical Laboratory Scientist (CLS) were replaced by Medical Laboratory Scientist, MLS(ASCP)CM. The BOC Board of Governors will be composed of five ASCP Fellows (pathologists), five ASCP laboratory professionals, four representatives of ASCLS, two representatives of the Association of Genetic Technologists, eight representatives from the eight participating societies respectively, and one public representative. The acquisition was criticized by AMT as doing little to further the standing of laboratory professionals. In 2021, ASCP acquired the Clinical Laboratory Management Association (CMLA). CMLA had advocated against laboratory personnel licensure as an unnecessary cost.
Sources: en.wikipedia.org
== Protection & Formation == Fmoc-carbamate is frequently used as a protecting group for primary and secondary amines, where the Fmoc group can be introduced by reacting the amine with fluorenylmethyloxycarbonyl chloride (Fmoc-Cl), e.g.:
==== Absorption ==== The absorption of atomoxetine with oral administration is rapid and complete. The drug's absolute bioavailability is 63 to 94%. This is moderated by first-pass metabolism and CYP2D6 status, with poor metabolizers having a bioavailability of 94% and extensive metabolizers having a bioavailability of 63%. Extensive metabolizers are considered to have normal CYP2D6 activity and constitute >90% of people, while poor metabolizers constitute a small minority of up to 7%. The bioavailability of atomoxetine is not different between capsule and solution forms. The time to peak levels of atomoxetine is 1 to 2 hours. It has been reported that the time to peak levels was 1.0 hours in CYP2D6 extensive metabolizers and 2.5 hours in CYP2D6 poor metabolizers. Taking atomoxetine with food does not affect its bioavailability or total exposure but decreases peak levels by 9% with a typical meal and 37% with a standard high-fat breakfast. In addition, food delays the time to peak levels by 3 hours. Atomoxetine exposure increases proportionally with higher doses over a range of 10 to 120 mg orally. Exposure to atomoxetine is proportional to body weight, and hence weight-normalizing dosing is required to produce equivalent exposure. In CYP2D6 poor metabolizers, atomoxetine peak levels are 5- to 6-fold higher and total exposure is 8- to 10-fold higher than in CYP2D6 extensive metabolizers.
=== Economics === In December 2019, the US FDA approved a generic version of apixaban produced jointly by Mylan and Micro Labs. BMS and Pfizer worked quickly to block generics from being created, and in August 2020, they won a patent infringement lawsuit against Sigmapharm, Sunshine Lake, and Unichem, after previously settling patent cases against 25 other companies. In September 2021, a Federal Circuit Court upheld the ruling. The result is that apixaban generics will most likely not be available in the United States until at least 2026, but possibly 2031. In July 2022, the Canadian generic drug company, Apotex Inc., obtained approval for marketing of apixaban. Pfizer reported revenue of US$6.747 billion for Eliquis in 2023. Apixaban is one of ten medications covered by price negotiations in the US under the Inflation Reduction Act. The negotiations, conducted by the Centers for Medicare & Medicaid Services, apply to pricing for Medicare recipients. The results of the negotiations were announced in August 2024, and Medicare's negotiated price for a 30-day supply of Eliquis is $231, a 56% decrease from the 2023 list price of $521. The pricing is set to take effect in 2026.
== In animals == The Biological Value method is also used for analysis in animals such as cattle, poultry, and various laboratory animals such as rats. It was used by the poultry industry to determine which mixtures of feed were utilized most efficiently by developing chicken. Although the process remains the same, the biological values of particular proteins in humans differs from their biological values in animals due to physiological variations.
Sources: en.wikipedia.org
metabolite An intermediate or end product of metabolism, especially degradative metabolism (catabolism); or any substance produced by or taking part in a metabolic reaction. Metabolites include a huge variety of small molecules generated by cells from various pathways and having various functions, including as inputs to other pathways and reactions, as signaling molecules, and as stimulators, inhibitors, and cofactors of enzymes. Metabolites may result from the degradation and elimination of naturally occurring compounds as well as of synthetic compounds such as pharmaceuticals.
=== Aspirational use as green chemicals === Natural polyphenols have long been proposed as renewable precursors to produce plastics or resins by polymerization with formaldehyde, as well as adhesives for particleboards. The aims are generally to make use of plant residues from grape, olive (called pomaces), or pecan shells left after processing.
=== Fish === A University of Florida scientist reports that male sand gobies work harder at building nests and taking care of eggs when females are present – the first time such "courtship parental care" has been documented in any species. In the cichlid species Tropheus moorii, a male and female will form a temporary monogamous pair bond and spawn; after which, the female leaves to mouthbrood the eggs on her own. T. moorii broods exhibit genetic monogamy (all eggs in a brood are fertilized by a single male). Another mouth brooding cichlid – the Lake Tanganyika cichlid (Xenotilapia rotundiventralis) has been shown that mating pairs maintain pair bonds at least until the shift of young from female to male. More recently the Australian Murray cod has been seen maintaining pair bonds over 3 years. Pair bonding may also have non-reproductive benefits, such as assisted resource defense. Recent study comparing two species of butterflyfishes, C. baronessa and C. lunulatus, indicate increase in food and energy reserves compared to individual fish.
Sources: en.wikipedia.org
Registered medical products are most often 0.1% nasal drops. Research suppliers ship lyophilized powder, usually in milligram quantities, which is dissolved before use. The active peptide is the same in both cases; presentation and excipients differ.
No. The peptide is synthetic, although it is modelled on a fragment of a naturally occurring hormone. ACTH(4-10) is generated when ACTH is cleaved, but the Pro-Gly-Pro extension is not a known endogenous sequence. It is therefore a designed analogue rather than a natural metabolite.
The label reflects reported effects on attention, memory and recovery after neurological injury in regional clinical reports. Those reports are mostly small and have not been widely replicated outside the region. The classification is descriptive and does not imply a single defined mechanism.
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。