This is a working overview of heptapeptide, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2026-02-20 and is reviewed periodically as new material appears.
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。
纯度评估以反相高效液相色谱为主，通过主峰面积百分比给出粗略结果，再配合电喷雾质谱核对分子量。氨基酸分析可验证组成比例，手性色谱或毛细管电泳用于检查残基构型。常见杂质包括缺失序列的短肽、氧化产物与二聚体。由于多数市售品不附带完整检验报告，独立第三方检测常被用来核实标称值。
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.
Later generations of the molecule include an N-acetylated form and an amidated form, both marketed online alongside the parent peptide. These variants differ in terminal chemistry and stability, and they are frequently discussed in the same breath even though they have not been compared in controlled trials. Supply outside formal healthcare systems comes largely from laboratories that synthesize peptides to order. Purity and identity of these materials vary widely, and no single body oversees the international trade.
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.
| 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 |
Lyophilised powder is normally kept at -20 °C in a desiccated container, with some suppliers recommending -80 °C for long-term archival storage. Repeated freeze-thaw cycles are the most common cause of avoidable loss, so aliquoting before freezing reduces variability between working sessions. Dissolved peptide is far less stable than the dry solid and is usually prepared fresh or held briefly at 4 °C. Aqueous solutions support both hydrolysis of the backbone and oxidation of the N-terminal methionine, and these two routes dominate degradation under ordinary laboratory conditions.
Identity and purity are confirmed with reversed-phase high-performance liquid chromatography, typically monitored at 214 nanometres where the peptide bond absorbs. Mass spectrometry, either electrospray or MALDI-TOF, verifies molecular mass against the theoretical value and detects truncation or adduct formation. Amino acid analysis and peptide mapping provide additional confirmation when required. The most frequently reported impurities are deletion sequences from incomplete coupling, methionine sulfoxide from oxidation, and dimeric species formed through non-covalent aggregation. Impurity profiles depend strongly on the synthesis and purification route chosen by the producer.
Published research has focused mainly on neurological and cognitive endpoints in animal models, with proposed mechanisms involving brain-derived neurotrophic factor and related signalling pathways. A substantial share of the human data originates from a limited number of research groups, and independent replication in other countries remains sparse. Regulatory status reflects that distribution: the peptide is registered as a medicine in Russia and appears in some neighbouring markets, while elsewhere it is handled as a research chemical without approved therapeutic labelling. Questions about dose-response relationships, long-term effects, and comparability across studies are still open.
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.
Clinical evidence consists largely of small trials with modest sample sizes, often without independent replication. Reported endpoints include cognitive scores, recovery after stroke, and visual function, but study designs vary widely and few trials meet contemporary reporting standards. Systematic reviewers have noted a high risk of bias in several of these reports. No large multicenter trial conducted outside Russia has been published. The compound is therefore best described as investigational in most jurisdictions, with its clinical role still unresolved.
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.
== Discovery of 2 active sites: C-domain and N-domain == Most of the ACE inhibitors on the market today are non-selective towards the two active sites of ACE because their binding to the enzyme is based mostly on the strong fundamental interaction between the zinc atom in the enzyme and the strong chelating group on the inhibitor. The resolution of the 3D structure of germinal ACE, which has only one active site that corresponds with C-domain of the somatic ACE, offers a structural framework for structure-based design approach. Although N- and C-domain have comparable rates in vitro of ACE hydrolyzing, it seems like that in vivo the C-domain is mainly responsible for regulating blood pressure. This indicates that C-domain selective inhibitors could have similar profile to that of a current non-selective inhibitors. Angiotensin I is mainly hydrolyzed by the C-domain in vivo but bradykinin is hydrolyzed by both active sites. Thus, by developing a C-domain selective inhibitor would permit some degradation of bradykinin by the N-domain and this degradation could be enough to prevent accumulation of excess bradykinin which has been observed during attacks of angioedema. C-domain selective inhibition could possibly result in specialized control of blood pressure with less vasodilator-related adverse effects. N-domain selective inhibitors on the other hand give the possibility of opening up novel therapeutic areas.
== Operation == The extraction cells consist of hollow bodies with inlets and outlets of liquid connection. The cells are first filled with the liquid chosen to be the stationary phase. Under rotation, the pumping of the mobile phase is started, which enters the cells from the inlet. When entering the flow of mobiles phase forms small droplets according to the Stokes' law, which is called atomization. These droplets fall through the stationary phase, creating a high interface area, which is called the extraction. At the end of the cells, these droplets unite due to the surface tension, which is called settling. When a sample mixture is injected as a plug into the flow of mobile phase the compounds of the mixtures elute according to their partition coefficients:
=== North America === Aruba (constituent country of the Netherlands): Flights to the United States were cancelled as a precautionary measure. Prime Minister Mike Eman stated that despite the island's geographic proximity to Venezuela, Aruba was "well prepared" and that there was no cause for concern for daily life to Arubans. The Bahamas: The Ministry of Foreign Affairs supported the Caribbean Community's position on the intervention and stressed that all parties should act in accordance with international law. The government also advised Bahamians not to travel to Venezuela because of the security situation. Canada: Minister of Foreign Affairs Anita Anand said that Canada refused to recognise the "illegitimate regime" of Maduro and opposed its "repression" of the Venezuelan people. She also stated that Canada calls on all parties to respect international law. Cuba: President and First Secretary of the Communist Party Miguel Díaz-Canel denounced "the criminal attack by the US" on Venezuela, and he called for urgent condemnation from the international community for what he described as "state terrorism against the brave Venezuelan people and against Our America". El Salvador: President Nayib Bukele posted a photo of a captured Maduro.
Under Maher's supervision, the 4th Armoured Division expanded captagon production and trafficking from Syria into a "business model controlled by the regime". In 2022, 90% of all Captagon pills manufactured in Syria exported by drug cartels affiliated with Assad regime arrived at its customer destinations across the world. Although hundreds of millions of pills were intercepted and seized by police forces, these accounted only for 10% of the total Captagon exports of the drug cartels linked to the Assad regime. In 2020, Italian police seized 84 million captagon pills originating from Syrian ports while intercepting a single shipment. In June 2023, US State Department's Bureau of Near Eastern Affairs published a detailed report to the US Congress, elucidating a strategy to eliminate the narcotics production, drug trafficking and drug cartel networks affiliated with the Assad regime and Hezbollah. A joint investigation conducted by Organized Crime and Corruption Reporting Project (OCCRP) and BBC News Arabic published a documentary in June 2023, revealing further details about the activities of regime officials, Ba'athist military commanders and Assad family members in their involvement in Syria's drug cartel. The investigation found that Lebanese criminal and drug kingpin Hassan Daqou collaborated with Syria's Fourth Armoured Division on trafficiking billions of dollars of drugs, under the command of General Ghassan Bilal, the right-hand man of Maher al-Assad. The report also unearthed Hezbollah's close participation in the drug production and smuggling networks.
Sources: en.wikipedia.org
=== Pharmacodynamics === Pinoline shows affinity for serotonin receptors, including the serotonin 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors (Ki = 156–4,335 nM). It is a high-efficacy partial agonist of the serotonin 5-HT2A receptor, an antagonist of the serotonin 5-HT2B receptor, and a full agonist of the serotonin 5-HT2C receptor, with EC50Tooltip half-maximal effective concentration (EmaxTooltip maximal efficacy) values of 2,140 nM (75%) at the serotonin 5-HT2A receptor and 33 nM (95%) at the serotonin 5-HT2C receptor and an IC50Tooltip half-maximal inhibitory concentration of 1,120 nM at the serotonin 5-HT2B receptor. Hence, pinoline appears to act as a potent and selective serotonin 5-HT2C receptor agonist. The drug shows affinity for the serotonin transporter (SERT) (Ki = 172–572 nM). It is a serotonin reuptake inhibitor, with an IC50 value of 1,100 nM. Pinoline shows affinity for the imidazoline I2 receptor (Ki = 1,640 nM) and for the α2-adrenergic receptor (Ki = 7,830 nM). Conversely, it shows no affinity for the dopamine D2 receptor (Ki = >10,000 nM). The drug is a weak monoamine oxidase inhibitor (MAOI), with an IC50 value for inhibition of MAO-ATooltip monoamine oxidase A of 41,500 nM. Both pinoline and tryptoline partially substitute for the psychedelic drug LSD in rodent drug discrimination tests. The substitution by tryptoline was further assessed and was found to be blocked by the serotonin receptor antagonist pizotifen and by the serotonin synthesis inhibitor para-chlorophenylalanine (PCPA).
As a consequence of the exchange rate policy, the bank must always adjust its interest rates to ensure a stable exchange rate and consequently cannot at the same time conduct monetary policy to stabilize e.g. domestic inflation or unemployment rates. This makes the conduct of stabilization policy fundamentally different from the situation in Denmark's neighbouring countries like Norway, Sweden, Poland and the United Kingdom, in which the central banks have a central stabilizing role. Denmark is presently the only OECD member country maintaining an independent currency with a fixed exchange rate. Consequently, the Danish krone is the only currency in the European Exchange Rate Mechanism II (ERM II), before Bulgaria and Croatia joined in 2020 (the latter uses the euro since 2023) In the first months of 2015, Denmark experienced the largest pressure against the fixed exchange rate for many years because of very large capital inflows, causing a tendency for the Danish krone to appreciate. Danmarks Nationalbank reacted in various ways, chiefly by lowering its interest rates to record low levels. On 6 February 2015 the certificates of deposit rate, one of the four official Danish central bank rates, was lowered to −0.75%. In January 2016 the rate was raised to −0.65%, at which level it has been maintained since then. Inflation in Denmark as measured by the official consumer price index of Statistics Denmark was 1.1% in 2017. Inflation has generally been low and stable for the last decades.
== Mechanism == Silanization mechanisms vary with substrate and with silanization reagent. In the usual circumstance, surface MOH groups react as nucleophiles with silyl chlorides or silyl alkoxides. The stoichiometry for these reactions are shown:
Sources: en.wikipedia.org
Secondary structure refers to highly regular local sub-structures on the actual polypeptide backbone chain. Two main types of secondary structure, the α-helix and the β-strand or β-sheets, were suggested in 1951 by Linus Pauling. These secondary structures are defined by patterns of hydrogen bonds between the main-chain peptide groups. They have a regular geometry, being constrained to specific values of the dihedral angles ψ and φ on the Ramachandran plot. Both the α-helix and the β-sheet represent a way of saturating all the hydrogen bond donors and acceptors in the peptide backbone. Some parts of the protein are ordered but do not form any regular structures. They should not be confused with random coil, an unfolded polypeptide chain lacking any fixed three-dimensional structure. Several sequential secondary structures may form a "supersecondary unit".
== Effect of pressure == At temperatures below 300 °C water is fairly incompressible, which means that pressure has little effect on the physical properties of water, provided it is sufficient to maintain a liquid state. This pressure is given by the saturated vapour pressure, and can be looked up in steam tables, or calculated. As a guide, the saturated vapour pressure at 121 °C is 200 kPa, 150 °C is 470 kPa, and 200 °C is 1550 kPa. The critical point is 21.7 MPa at a temperature of 374 °C, above which water is supercritical rather than superheated. Above about 300 °C, water starts to behave as a near-critical liquid, and physical properties such as density start to change more significantly with pressure. However, higher pressures increase the rate of extractions using superheated water below 300 °C. This could be due to effects on the substrate, particularly plant materials, rather than changing water properties.
The molecular weight of prothrombin is approximately 72,000 Da. The catalytic domain is released from prothrombin fragment 1.2 to create the active enzyme thrombin, which has a molecular weight of 36,000 Da. Structurally, it is a member of the large PA clan of proteases. Prothrombin is composed of four domains; an N-terminal Gla domain, two kringle domains and a C-terminal trypsin-like serine protease domain. Factor Xa with factor V as a cofactor leads to cleavage of the Gla and two Kringle domains (forming together a fragment called fragment 1.2) and leave thrombin, consisting solely of the serine protease domain. As is the case for all serine proteases, prothrombin is converted to active thrombin by proteolysis of an internal peptide bond, exposing a new N-terminal Ile-NH3. The historic model of activation of serine proteases involves insertion of this newly formed N-terminus of the heavy chain into the β-barrel promoting the correct conformation of the catalytic residues. Contrary to crystal structures of active thrombin, hydrogen-deuterium exchange mass spectrometry studies indicate that this N-terminal Ile-NH3 does not become inserted into the β-barrel in the apo form of thrombin. However, binding of the active fragment of thrombomodulin appears to allosterically promote the active conformation of thrombin by inserting this N-terminal region.
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 originated at the Institute of Molecular Genetics in Moscow during the 1980s. The work was carried out by a Russian research group that specialized in peptide neuropharmacology.