A practical reference on ACTH analog: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2025-12-21. Anything still debated is marked as such rather than presented as settled.
从分子层面看，Semax 是线性七肽，没有二硫键、糖基或脂链修饰，N 端为游离氨基，C 端为游离羧基。分子含组氨酸与谷氨酸侧链，因此在水和甲醇等极性溶剂中溶解良好，在非极性溶剂中溶解有限。计算分子量约为 814 Da，与其质子化离子的质荷比吻合，可用于质谱确认。
稳定性主要由水解与氧化两条路径支配。肽键在中性或弱酸性条件下相对稳定，遇到强碱或长时间高温则明显断裂；甲硫氨酸侧链容易被氧化成亚砜，使主峰前移并拉低实际含量。金属离子、光照和反复冻融会进一步促进降解或聚集。冻干粉在低温避光条件下可存放较长时间，配制后的水溶液通常需要冷藏并尽快用完。
Development is attributed to researchers at the Institute of Molecular Genetics in Moscow during the early 1980s, building on earlier Soviet work with ACTH fragments. Russian regulatory approval followed for intranasal use, and the compound has remained commercially available there for decades. Most published human data originate from Russian and, later, some Eastern European clinical reports, which are not always accessible in English translation. Outside that region the material is generally handled as a research chemical rather than a licensed medicine.
Regulatory status differs sharply between jurisdictions. In Russia the peptide is registered as a prescription nasal preparation, while agencies such as the United States Food and Drug Administration have not approved it for any indication. Products sold elsewhere are typically labeled for laboratory research only, and such labels shift responsibility for safe handling to the purchaser. Because the same name covers pharmaceutical-grade nasal drops and bulk research powder, identity and purity documentation becomes the main practical concern when comparing sources.
Semax is a synthetic seven-amino-acid peptide whose sequence extends the ACTH(4-10) fragment with a C-terminal proline-glycine-proline tripeptide. The commonly cited sequence is Met-Glu-His-Phe-Pro-Gly-Pro, giving a molecular formula near C37H51N9O10S and a molecular weight close to 813.9 g/mol. It belongs to the broader class of synthetic ACTH fragments studied for central nervous system effects rather than for adrenal steroid stimulation. In practice the material appears as a lyophilized white powder for laboratory work or as a dilute saline solution in clinical settings.
| Property | Value | Notes |
|---|---|---|
| 分子式 | C37H51N9O10S | 游离碱形式 |
| 等电点 | 约 6.5 | 估算值，随缓冲体系变化 |
| 主要降解途径 | 水解与氧化 | 侧链氧化最为常见 |
| 溶液储存 | 2 至 8 摄氏度避光 | 避免反复冻融 |
| 常规分析手段 | 反相色谱与质谱联用 | 氨基酸分析辅助核对 |
Identity and purity of Semax are established mainly by reversed-phase high-performance liquid chromatography coupled with mass spectrometry. The chromatographic trace gives a purity estimate as a percentage of total peak area, while electrospray or matrix-assisted laser desorption ionization confirms the molecular mass against the calculated value. Amino acid analysis and sequence-specific fragmentation provide further confirmation when a supplier's chain of custody is unclear. Vendors frequently quote a purity figure without stating the detection wavelength or the integration method, which limits how far one number can be compared with another.
Stability depends heavily on physical state. Lyophilized powder held dry, cold and dark retains its content over long periods, whereas dissolved peptide begins to change within days at room temperature. The most cited degradation route is oxidation of the methionine residue, which converts the peptide to a sulfoxide form that elutes differently on chromatography. Hydrolysis of amide bonds and adsorption onto container walls contribute smaller losses. Buffers that exclude oxygen from the headspace slow the oxidation pathway, but no single condition prevents all change indefinitely.
Practical handling follows from those properties. Bulk material is best divided into single-use portions soon after receipt, because each thaw exposes the whole container to moisture and temperature cycling. Vials should be allowed to reach room temperature before opening to prevent condensation on the powder. Low-binding plasticware reduces loss of dilute solutions, and sterile filtration is used when a preparation must remain free of microbial growth. Records of batch number, reconstitution date and storage history are what allow a later analytical result to be interpreted meaningfully.
Semax is a synthetic heptapeptide whose sequence is Met-Glu-His-Phe-Pro-Gly-Pro. The first four residues correspond to the ACTH(4-10) fragment, while the terminal Pro-Gly-Pro extension was added to improve metabolic stability. Its molecular formula is C37H51N9O10S and its monoisotopic mass is approximately 813.9 Da. The compound is classified as a peptide research chemical and as a registered pharmaceutical product in Russia, but it does not hold marketing approval in the European Union or the United States. Naming conventions vary across supplier catalogs.
Development of the compound took place in the Soviet Union during the 1980s, largely through peptide research groups affiliated with the Shemyakin-Ovchinnikov Institute and Moscow State University. Investigators screened fragments of adrenocorticotropic hormone for activity on the central nervous system while attempting to separate cognitive effects from hormonal ones. The shortened sequence was selected because it retained behavioral activity in animal models without stimulating corticosteroid release. Early publications described the molecule as an ACTH(4-10) analog.
Published research on this peptide originates mainly from Russian laboratories, and the wider international literature is comparatively thin. Studies have used rodent models of stroke, hypoxia, and memory tasks, with a smaller number of human trials reported. Reported outcomes include changes in attention and memory measures, along with effects on neurotrophic factor expression in some experiments. Small sample sizes, inconsistent dosing protocols, and limited independent replication are widely noted limitations, so the strength of the clinical evidence remains an open question.
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.
Semax is a synthetic heptapeptide developed in the Soviet Union during the 1980s by researchers at the Institute of Molecular Genetics in Moscow. It was designed as a truncated analog of adrenocorticotropic hormone, retaining only the fragment spanning residues four through ten. Investigators sought a peptide that would preserve the cognitive effects associated with ACTH while eliminating the hormonal stimulation of the adrenal cortex. The compound entered clinical use in Russia during the following decade.
Russian regulatory authorities approved the peptide for nasal administration, and it remains listed in the national pharmacopoeia under several trade names. Documented indications include acute ischemic stroke, transient ischemic attacks, traumatic brain injury, and certain ophthalmological and neurological conditions. Physicians also prescribe it for cognitive complaints in older patients, although the evidence base for that use is thinner. Outside Russia and a few neighboring states, the substance is not an approved medicine and is sold instead as a research chemical.
Potentiometric and/or spectrophotometric data: PSEQUAD Potentiometric data: HYPERQUAD, BEST, ReactLab pH PRO Spectrophotometric data: HypSpec, SQUAD, SPECFIT, ReactLab EQUILIBRIA., suprafit NMR data HypNMR, WINEQNMR2 Archived 2019-07-14 at the Wayback Machine, suprafit In biochemistry, formation constants of adducts may be obtained from Isothermal titration calorimetry (ITC) measurements. This technique yields both the stability constant and the standard enthalpy change for the equilibrium. It is mostly limited, by availability of software, to complexes of 1:1 stoichiometry.
==== Plasmid delivery ==== Individual genes can be inserted into specific sites on plasmids, and recombinant plasmids can be introduced into living cells. A method using macro-branched TAT has been proposed for plasmid DNA delivery into various cell lines and showed significant transfection capabilities. Multimers of TAT have been found to increase transfection efficiency of plasmid DNA by 6-8 times more than poly-L-arginine or mutant TAT2-M1, and by 390 times compared with the standard vectors.
These receptors modulate the release of other neurochemicals such as serotonin in the case of MOR agonists, and acetylcholine in the case of D2. These changes can account for the physical and psychological remission of the pathology of addiction. The longer effects of KOR agonism (30 minutes or greater) have been linked to KOR-dependent stress-induced potentiation and reinstatement of drug seeking. It is hypothesized that these behaviors are mediated by KOR-dependent modulation of dopamine, serotonin, or norepinephrine and/or via activation of downstream signal transduction pathways. Of significant note, while KOR activation blocks many of the behavioral and neurochemical responses elicited by drugs of abuse as stated above. These results are indicative of the KOR induced negative affective states counteracting the rewarding effects of drugs of abuse. Implicating the KOR/dynorphin system as an anti-reward system, supported by the role of KOR signaling and stress, mediating both stress-induced potentiation of drug reward and stress-induced reinstatement of seeking behavior. This in turn addresses what was thought to be paradoxical above. That is, rather, KOR signaling is activated/upregulated by stress, drugs of abuse and agonist administration - resulting in negative affective state. As such drug addiction is maintained by avoidance of negative affective states in stress, craving, and drug withdrawal.
In 1804 the Balmis Expedition, an official Spanish mission commanded by Francisco Javier de Balmis, sailed to spread the vaccine throughout the Spanish Empire, first to the Canary Islands and on to Spanish Central America. While his deputy, José Salvany, took vaccine to the west and east coasts of Spanish South America, Balmis sailed to Manila in the Philippines and on to Canton and Macao on the Chinese coast. He returned to Spain in 1806. The vaccine was not carried in the form of flasks, but in the form of 22 orphaned boys, who were 'carriers' of the live cowpox virus. After arrival, "other Spanish governors and doctors used enslaved girls to move the virus between islands, using lymph fluid harvested from them to inoculate their local populations". Napoleon was an early proponent of smallpox vaccination and ordered that army recruits be given the vaccine. Additionally a vaccination program was created for the French Army and his Imperial Guard. In 1811 he had his son, Napoleon II, vaccinated after his birth. By 1815 about half of French children were vaccinated and by the end of the Napoleonic Empire smallpox deaths accounted for 1.8% of deaths, as opposed to the 4.8% of deaths it accounted for at the time of the French Revolution. On March 26, 1806, the Swiss canton Thurgau became the first state in the world to introduce compulsory smallpox vaccinations, by order of the cantonal councillor Jakob Christoph Scherb. Half a year later, Elisa Bonaparte issued a corresponding order for her Principality of Lucca and Piombino on 25 December 1806.
Sources: en.wikipedia.org
==== Congress of South African Students ==== Accounts of the uprising typically accord a central role to black young adults – known in the anti-apartheid movement as "young lions" or "comrades" – who became the "shock troops" of the revolt. Their largest and most prominent organisational base was COSAS, another UDF affiliate that was founded in 1979, with a local branch in Vaal from March 1980. COSAS apparently played an important role in politicising the youth of Vaal, including by encouraging them to support the VCA, and many of the most militant participants in the uprising were formally or informally affiliated to COSAS.
=== 5S-GlcNAc === Ac45S-GlcNAc is converted intracellularly into UDP-5S-GlcNAc, a substrate analogue inhibitor of OGT. UDP-5S-GlcNAc is not efficiently utilized as a donor sugar by OGT, possibly due to distortion of the pyranose ring by replacement of oxygen with sulfur. As other glycosyltransferases utilize UDP-GlcNAc as a donor sugar, UDP-5S-GlcNAc has some non-specific effects on cell-surface glycosylation.
Myeloproliferative disease (primarily essential thrombocythemia and polycythemia vera). It has been found to be superior to anagrelide for the control of ET. Sickle-cell disease (increases production of fetal hemoglobin that then interferes with the hemoglobin polymerisation as well as by reducing white blood cells that contribute to the general inflammatory state in sickle cell patients.) Second line treatment for psoriasis (slows down the rapid division of skin cells) Systemic mastocytosis with associated hematological neoplasm(SM-AHN) (The utility in treating SM-AHN with hydroxycarbamide stems from its myelosuppressive activity, it does not however exhibit any selective anti-mast cell activity) Chronic myelogenous leukemia (largely replaced by imatinib, but still in use for its cost-effectiveness)
Sources: en.wikipedia.org
[b]oth hot-iron and freeze branding cause acute pain in the first 1.5 h after branding as shown by the marked increase in cortisol. The more pronounced and prolonged elevation of cortisol observed in H animals implies that hot-iron branding may be initially (up to 40 min after branding) more distressing than freeze branding. However, there appeared to be no differences after the 40 min sampling time suggesting that the discomfort caused by both methods is relatively short lived.
=== Diabetes Mellitus === Increased levels of proinsulin in the circulatory system relative to mature insulin concentrations can indicate impending insulin resistance and the development of type 2 diabetes. Additional problems with proinsulin that can lead to diabetes include mutations in the number of cysteines present, which could affect correct folding. If the mutation causes only a mild change it could simply stress the endoplasmic reticulum’s ability to properly fold the protein. This stress, after a while, would lead to a decrease in the number of β-cells producing mature insulin, and would then lead to diabetes mellitus.
An economical semisynthesis of progesterone from the plant steroid diosgenin isolated from yams was developed by Russell Marker in 1940 for the Parke-Davis pharmaceutical company. This synthesis is known as the Marker degradation.
Sources: en.wikipedia.org
电喷雾或基质辅助激光解吸电离质谱是常用手段，测得的质子化离子质荷比可换算为分子量。结果与理论值落在合理误差内，才支持结构一致的判断。
甲硫氨酸侧链含硫醚，在氧气、光照或金属离子存在时容易被氧化。氧化产物极性略增，常在色谱图上表现为主峰之前的肩峰或前伸峰。
通常建议冷藏避光，并在较短时间内使用。不存在适用于所有配方的统一期限，具体取决于浓度、缓冲体系与容器材质。
It is a short synthetic peptide built from seven amino acids: methionine, glutamic acid, histidine, phenylalanine and three prolines. The sequence derives from the 4-10 fragment of adrenocorticotropic hormone with an added proline-glycine-proline tail. No plant or animal extract is involved; the material is produced by solid-phase peptide synthesis.