A practical reference on 鼻内给药: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2025-11-24. Anything still debated is marked as such rather than presented as settled.
Reported pharmacological work centers on neurotrophic signaling, including changes in BDNF and NGF expression in hippocampal tissue in animal models. Human data come largely from studies conducted in Russia, and how well those results generalize to other populations remains an open question. Regulatory status differs sharply by jurisdiction: Semax is a registered prescription medicine in Russia, while it holds no approved marketing status in the United States or the European Union. Outside such jurisdictions it is generally handled as a research chemical, which affects both documentation and quality expectations.
Semax is a synthetic heptapeptide whose sequence is Met-Glu-His-Phe-Pro-Gly-Pro. It was developed as a fragment analog of adrenocorticotropic hormone, modeled specifically on the ACTH(4-10) region. The first four residues reproduce that fragment, while a Pro-Gly-Pro tripeptide is appended at the C-terminus. Work on the compound originated in Russia, where it entered clinical use as an intranasal preparation. Its sequence places it among short regulatory peptides studied for effects on the central nervous system rather than on the adrenal axis.
The C-terminal Pro-Gly-Pro extension is not incidental. Proline-rich tails are known to resist several common peptidases, and the published literature attributes the longer half-life of Semax, relative to unmodified ACTH fragments, to this feature. The modification also removes the melanocyte-stimulating and corticosteroidogenic activity that characterizes longer ACTH-derived sequences. Because the molecule is small and hydrophilic, it is typically formulated as an aqueous solution for intranasal or parenteral delivery. Acetylation or amidation at the termini appears in closely related research peptides and shifts the mass by a fixed increment.
Semax is a synthetic heptapeptide with the sequence Met-Glu-His-Phe-Pro-Gly-Pro. Its chain combines the first seven residues of corticotropin with a C-terminal proline-glycine-proline extension, a modification intended to slow enzymatic breakdown. The free peptide has a molecular mass near 813.9 daltons. It belongs to the class of ACTH-derived fragments studied for central nervous system activity rather than for adrenal steroid stimulation. This structural relationship to a natural hormone fragment is the usual starting point for describing the compound in the literature.
Development took place during the 1980s at institutes of the Russian Academy of Sciences, where peptide fragments of ACTH were screened for cognitive and neuroprotective effects. The compound received regulatory approval in Russia as a nasal preparation, marketed for conditions such as ischemic stroke, transient ischemic attacks, and optic nerve disorders. Registration in other countries has not followed. Most published clinical reports originate from a small number of Russian research groups, and independent replication outside that setting remains limited. The regulatory status therefore differs sharply between Russia and the rest of the world.
Laboratory work points toward modulation of neurotrophic signaling, particularly expression of brain-derived neurotrophic factor and nerve growth factor in hippocampal tissue. Studies also describe effects on monoamine turnover, inflammatory mediators, and oxidative markers. These observations come mainly from animal models and cultured cells, so the causal chain in humans is not firmly established. Whether the reported molecular changes translate into measurable clinical benefit is an open question. Reviews generally present the mechanism as plausible rather than demonstrated.
| Property | Value | Notes |
|---|---|---|
| Molecular weight | ~813.9 Da (free heptapeptide) | N-acetylated form is about 42 Da heavier |
| Residue count | 7 (heptapeptide) | Four residues from ACTH(4-10), three added |
| Appearance | White to off-white powder | Usually supplied lyophilized |
| Solubility class | Freely soluble in water | Also dissolves in DMSO and polar organic solvents |
| Related parent fragment | ACTH(4-10) | Parent motif is Met-Glu-His-Phe |
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。
Anhydrous hydrogen bromide is a poor solvent, only able to dissolve small molecular compounds such as nitrosyl chloride and phenol, or salts with very low lattice energies such as tetraalkylammonium halides.
Quinolones are chemotherapeutic bactericidal drugs. They interfere with DNA replication by preventing bacterial DNA from unwinding and duplicating. Specifically, they inhibit the ligase activity of the type II topoisomerases, DNA gyrase and topoisomerase IV, which cut DNA to introduce supercoiling, while leaving nuclease activity unaffected. With the ligase activity disrupted, these enzymes release DNA with single- and double-strand breaks that lead to cell death. The majority of quinolones in clinical use are fluoroquinolones, which have a fluorine atom attached to the central ring system, typically at the 6-position or C-8 position. Most of them are named with the -oxacin suffix. First and second generation quinolones are largely active against Gram-negative bacteria, whereas third and fourth generation quinolones have increased activity against Gram-positive and anaerobic bacteria. Some quinolones containing aromatic substituents at their C-7 positions are highly active against eukaryotic type II topoisomerase. It has also been proposed that quinolone antibiotics cause oxidation of guanine nucleotides in the bacterial nucleotide pool, and that this process contributes to the cytotoxicity of these agents. The incorporation of oxidized guanine nucleotides into DNA could be bactericidal. Bacterial cytotoxicity could arise from incomplete repair of closely spaced 8-oxo-2'-deoxyguanosine in the DNA resulting in double-strand breaks.
FSL have been used to create human red cell kodecytes that have been used to detect and identify blood group allo-antibodies as ABO sub-group mimics, ABO quality control systems, serologic teaching kits and a syphilis diagnostic. Kodecytes have also demonstrated that FSL-FLRO4 is a suitable reagent for labelling packed red blood cells (PRBC) at any point during routine storage and look to facilitate the development of immunoassays and transfusion models focused on addressing the mechanisms involved in transfusion-related immunomodulation (TRIM). Murine kodecytes have been experimentally used to determine in vivo cell survival, and create model transfusion reactions. Zebrafish kodecytes have been used to determine real time in vivo cell migration. Kodecytes have been used to create influenza diagnostics. Kodecytes which have been modified with FSL-GB3 were unable to be infected with the HIV virus.
=== Toxicity === In 2009, one case of sympathomimetic toxicity was reported in the UK after a person took 0.2 g of mephedrone orally, and after this did not achieve the desired effect, intramuscularly injected 3.8 g mixed with water into his thighs. Shortly afterwards, the user "developed palpitations, blurred tunnel vision, chest pressure and sweating". The patient was treated with 1 mg of lorazepam and the sympathomimetic features decreased and the user was discharged within six hours of arrival. One case of serotonin syndrome has been reported, where the patient was already prescribed fluoxetine and olanzapine, and then took 40 tablets containing mephedrone in one night. He was treated with lorazepam and discharged 15 hours after admission. Both enantiomers of methcathinone, which differs only in the lack of the methyl group on the phenyl ring when compared to mephedrone, have been shown to be toxic to rat dopamine neurons, and the S-enantiomer was also toxic against serotonin neurons. Simon Gibbons and Mire Zloh of the School of Pharmacy, University of London stated, based on the chemical similarities between methcathinone and mephedrone, "it is highly likely that mephedrone will display neurotoxicity". However, Brunt and colleagues stated, "extreme caution" should be used when inferring the toxicity of mephedrone from methcathinone, noting some of the toxicity associated with methcathinone is due to manganese impurities related to its synthesis, rather than the compound itself.
Alfred Zack Gilman (February 5, 1908 – January 13, 1984) was an American pharmacologist best known for pioneering early chemotherapy techniques using nitrogen mustard with his colleague, Louis S. Goodman. The pair also published the classic textbook The Pharmacological Basis of Therapeutics in 1941, and Gilman served as an editor for its first six editions. Gilman served on the faculties of the Yale School of Medicine, the Columbia College of Physicians and Surgeons, and the Albert Einstein College of Medicine, where he founded the Department of Pharmacology. He was a member of U.S. National Academy of Sciences.
Sources: en.wikipedia.org
=== Oxides === Neptunium has two stable oxides, which are NpO2 and Np2O5. Np3O8 was reported in earlier literatures, though some studies suggesting that claims of Np3O8 are actually the result of mistaken analysis of Np2O5. The existence of another oxide Np4O9 has been suggested, but it has not been fully characterized. Although neptunium oxides have not been produced with neptunium in oxidation states as high as those possible with the adjacent actinide uranium, neptunium oxides are more stable at lower oxidation states. This behavior is illustrated by the fact that NpO2 can be produced by simply burning neptunium salts of oxyacids in air. The greenish-brown NpO2 is very stable over a large range of pressures and temperatures and does not undergo phase transitions at low temperatures. It does show a phase transition from face-centered cubic to orthorhombic at around 33–37 GPa, although it returns to its original phase when pressure is released. It remains stable under oxygen pressures up to 2.84 MPa and temperatures up to 400 °C. Np2O5 is black-brown in color and monoclinic with a lattice size of 418×658×409 picometres. It is relatively unstable and decomposes to NpO2 and O2 at 420–695 °C. Although Np2O5 was initially subject to several studies that claimed to produce it with mutually contradictory methods, it was eventually prepared successfully by heating neptunium peroxide to 300–350 °C for 2–3 hours or by heating it under a layer of water in an ampoule at 180 °C.
=== Recommendations === The IEEE standard 1188–1996 recommends replacing lithium-ion batteries in an electric vehicle, when their charge capacity drops to 80% of the nominal value. In what follows, we shall use the 20% capacity loss as a comparison point between different studies. We shall note, nevertheless, that the linear model of degradation (the constant % of charge loss per cycle or per calendar time) is not always applicable, and that a "knee point", observed as a change of the slope, and related to the change of the main degradation mechanism, is often observed.
Along with most of the Commonwealth and Allied nations, Southern Rhodesia sent a delegation of soldiers, airmen and seamen to London to take part in the grand Victory Parade of 8 June 1946. The colony's contingent, led by Colonel R E B Long, marched after South Africa and before Newfoundland. The Southern Rhodesian colour guard comprised a white officer and two black sergeants of the Rhodesian African Rifles. During the royal visit to Southern Rhodesia in April 1947, King George VI accorded the prefix "Royal" to the Rhodesia Regiment in recognition of its contributions to the two World Wars, and agreed to be its Colonel-in-Chief.
=== Genetics === Genetics plays a major role in fibromyalgia and may explain up to 50% of disease susceptibility. Fibromyalgia is potentially associated with polymorphisms of genes in the serotonergic, dopaminergic and catecholaminergic systems. Several genes have been suggested as candidates for susceptibility to fibromyalgia. These include a coding variation in Huntingtin, SLC6A4, TRPV2, MYT1L, NRXN3, and the 5-HT2A receptor 102T/C polymorphism. The heritability of fibromyalgia is estimated to be higher in patients younger than 50. Nearly all the genes suggested as potential risk factors for fibromyalgia are associated with neurotransmitters and their receptors.
Sources: en.wikipedia.org
The sequence is Met-Glu-His-Phe-Pro-Gly-Pro, a seven-residue peptide. The first four residues correspond to the ACTH(4-10) fragment, and Pro-Gly-Pro is added at the C-terminus. N-acetylated versions also appear in the literature and differ in mass.
Semax is a synthetic analog of the ACTH(4-10) fragment rather than a copy of the full hormone. Truncation plus the added tail removes the steroidogenic portion of ACTH. That distinction explains why it is studied for nervous-system effects instead of adrenal stimulation.
It is registered as a prescription product in Russia and has been used there clinically, chiefly by the intranasal route. No approval exists in the United States or the European Union. Availability elsewhere typically falls under research-chemical distribution, with varying purity documentation.
Semax is a synthetic seven-amino-acid peptide derived from a fragment of corticotropin. It is used in Russia as a nasal preparation, while elsewhere it is studied as a research compound. It is not approved as a medicine in most countries.