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� ”发背景与监管地位 — Explained

By Editorial Desk · published 2026-03-31 · last reviewed 2026-05-09 · Info

The short version of ACTH 片段 fits in a sentence. The long version — which is the one that helps — is below.

Reviewed 2026-05-09. Anything still debated is marked as such rather than presented as settled.

研发背景与监管地位

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。

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 Background and Molecular Structure

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 at a glance

PropertyValueNotes
结构类别线性合成七肽无环化结构,不含二硫键
氨基酸序列Met-Glu-His-Phe-Pro-Gly-ProN 端为甲硫氨酸
分子量约 814 Da游离碱形式的计算值
外观白色至类白色粉末具吸湿性
溶解性易溶于水亦可溶于甲醇等极性溶剂

Semax Structure and Research Background

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.

Related pages on this site

Supporting material

== Metabolism == Metabolism of 1,3-dibromopropane was examined in 1981. The examination was done by orally administering 1,3-dibromopropane to rats and collecting results 24 hours after administration. Results were obtained from three sources: urine, faeces, and expired air. Upon analysis of the urinary results, researchers discovered the formation of metabolite, N-acetyl-S-(1-bromo-3-propyl)-cysteine and the decline in the GSH content of the liver of the rats. This led to the assumption that 1,3-dibromopropane could have reacted with GSH after administration and gave rise to 1-bromo-3-propyl-S-glutathione, which ultimately form the urinary metabolite. Moreover, due to little radioactivity observed from feces and the confirmation from maintained blood levels of radioactivity proved the occurrence of biliary excretion of sulfur-containing metabolites and enterohepatic cycling.

In general, most actinide isotopes with an odd neutron number are fissile. Most nuclear fuels have an odd atomic mass number (A = Z + N = the total number of nucleons), and an even atomic number Z. This implies an odd number of neutrons. Isotopes with an odd number of neutrons gain an extra 1 to 2 MeV of energy from absorbing an extra neutron, from the pairing effect which favors even numbers of both neutrons and protons. This energy is enough to supply the needed extra energy for fission by slower neutrons, which is important for making fissionable isotopes also fissile. More generally, nuclides with an even number of protons and an even number of neutrons, and located near a well-known curve in nuclear physics of atomic number vs. atomic mass number are more stable than others; hence, they are less likely to undergo fission. They are more likely to "ignore" the neutron and let it go on its way, or else to absorb the neutron but without gaining enough energy from the process to deform the nucleus enough for it to fission. These "even-even" isotopes are also less likely to undergo spontaneous fission, and they also have relatively much longer partial half-lives for alpha or beta decay. Examples of these isotopes are uranium-238 and thorium-232.

Estradiol is available in the form of transdermal emulsions (e.g., Estrasorb) and sprays (e.g., Lenzetto, Evamist). Estradiol emulsions and sprays are administered daily. The pharmacokinetics of these preparations have been studied.

Sources: en.wikipedia.org

Notes from published material

A natriuretic peptide is a hormone molecule that plays a crucial role in the regulation of the cardiovascular system. These hormones were first discovered in the 1980s and were found to have very strong diuretic, natriuretic, and vasodilatory effects. There are three main types of natriuretic peptides: atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and C-type natriuretic peptide (CNP). Two minor hormones include urodilatin (URO) which is processed in the kidney and encoded by the same gene as ANP, and dendroaspis NP (DNP) that was discovered through isolation of the venom from the green mamba snake. Since they are activated during heart failure, they are important for the protection of the heart and its tissues. Additionally, there are three natriuretic peptide receptors: natriuretic peptide receptor A (NPR-A), Natriuretic Peptide Receptor-B (NPR-B), and Natriuretic Peptide Receptor-C (NPR-C). NPR-A and NPR-B use cyclic guanosine monophosphate (cGMP) as its intracellular messenger. NPR-A binds selectively to ANP and BNP while NPR-B binds selectively to CNP. Although initially thought to have no signaling activity, NPR-C is now believed to inhibit cyclic adenosine monophosphate (cAMP) using the Giα subunit along with activating phospholipase C-β using the Giβγ subunit. The three natriuretic peptides ANP, BNP, and CNP can bind to NPR-C however it has a higher affinity towards ANP and CNP. Natriuretic peptides will lose their activity when degraded by the enzyme neprilysin which is found on the plasma membrane.

The U.S. Justice Department considers the Mexican drug cartels to be the "greatest organized crime threat to the United States." In seeking partnership from the United States, Mexican officials point out that the illicit drug trade is a shared problem in need of a shared solution, and remark that most of the financing for the Mexican traffickers comes from American drug consumers. On March 25, 2009, U.S. Secretary of State Hillary Clinton stated that "[America's] insatiable demand for illegal drugs fuels the drug trade", and that "the United States bears shared responsibility for the drug-fueled violence sweeping Mexico." U.S. State Department officials knew that Mexican ex-president Felipe Calderón's willingness to work with the United States was unprecedented on issues of security, crime and drugs, so the U.S. Congress passed legislation in late June 2008 to provide Mexico and Central American countries with US$1.6 billion for the Mérida Initiative, a three-year international assistance plan that provides law enforcement training and equipment, as well as technical advice to strengthen the national justice systems. Under the Foreign Narcotics Kingpin Designation Act, the United States has sanctioned numerous Mexican drug traffickers and organizations by freezing assets and prohibiting financial transactions with them. Currently, the Mexican drug cartels already have a presence in most major U.S. cities.

Stretching of the atrial wall, via Atrial volume receptors Increased Sympathetic stimulation of β-adrenoceptors Increased sodium concentration (hypernatremia), though sodium concentration is not the direct stimulus for increased ANP secretion Endothelin, a potent vasoconstrictor Recently, it was discovered that ANP also can be O-glycosylated.

Sources: en.wikipedia.org

Frequently asked questions

Semax 在自然界中存在吗?

不存在。它是依据 ACTH 的一段序列人工设计的分子,天然蛋白质中找不到与之完全相同的七肽。名称属于研究代号,而非天然物质名。

它与 ACTH 的差别在哪里?

Semax 对应 ACTH 第 4 至第 10 位的片段,并在两端做了替换与延长,使其不再具备促肾上腺皮质激素的典型内分泌活性。这一改动同时改变了它在体内的稳定性与分布特征。

哪些地区可以合法获得?

俄罗斯将其列为处方药物,需要医生开具处方。多数其他国家把它当作研究化合物,不能作为药品销售或宣称疗效。具体合法性取决于当地法规。

What is the amino acid sequence of Semax?

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.

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