trans-3-hexenoyl raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.
This page was last updated on 2025-12-02 and is reviewed periodically as new material appears.
Tesamorelin is a synthetic peptide that belongs to the growth hormone-releasing hormone family and contains the same forty-four amino acid sequence as endogenous GHRH, extended at the amino terminus by a trans-3-hexenoyl group. That small fatty acid modification protects the peptide from rapid cleavage by dipeptidyl peptidase-4, the enzyme that shortens the half-life of native GHRH to only a few minutes. Chemically the compound is produced by solid-phase peptide synthesis, purified by chromatography, and supplied as a sterile lyophilized powder for reconstitution.
Regulatory approval in the United States came in 2010, when the Food and Drug Administration cleared the peptide for the reduction of excess abdominal fat in adults with HIV infection and associated lipodystrophy. The decision rested mainly on two randomized phase 3 trials that enrolled roughly eight hundred patients and ran for twenty-six weeks. Participants receiving active drug showed substantially greater declines in visceral adipose tissue than those receiving placebo, while total body weight changed comparatively little. A reformulated presentation was later approved, and the product has remained a niche therapy rather than a general weight-loss agent.
Tesamorelin occupies a narrow position among agents that act on the growth hormone axis. Unlike growth hormone itself, which is given as replacement, it stimulates the pituitary to release the hormone in pulses, so the downstream increase in insulin-like growth factor 1 depends on intact somatotroph function. Other peptides in the same family include shorter GHRH fragments and synthetic secretagogues with different stability profiles. Several points remain unresolved, including whether the reduction in visceral fat translates into fewer cardiovascular events, what happens to metabolic markers after long-term use, and how the drug compares with lifestyle or surgical approaches.
监管记录显示,特沙莫瑞林于 2010 年在美国首次获得批准,用于人类免疫缺陷病毒感染相关的脂肪营养不良患者。批准依据来自降低内脏脂肪的临床试验,而非体重或瘦体重的普遍改善。后续出现了不同制剂版本,但其核心适应症保持一致。关于长期心血管结局和死亡率影响,现有证据仍不充分。
在临床研究之外,特沙莫瑞林常被讨论为生长激素分泌促进剂,但这一说法需要限定。它并不等同于生长激素本身,也不属于普通减重药物。部分研究关注其减少腹部脂肪和改善脂质谱的潜力,另一些研究则关注胰岛素抵抗和 IGF-1 升高等信号。这些效应的临床意义仍在评估中,尚未形成统一结论。
| Property | Value | Notes |
|---|---|---|
| Peptide class | Synthetic GHRH analogue | 44 residues; N-terminal trans-3-hexenoyl group |
| First approval year | 2010 | United States; HIV-associated abdominal fat accumulation |
| Administration route | Subcutaneous injection | Abdominal site; clinician-administered or self-injected |
| Common synonyms | TH9507; tesamorelin acetate | Development code and acetate salt form |
| Originator | Canadian biotechnology firm | Original developer and regulatory sponsor |
Tesamorelin is a synthetic peptide that belongs to the growth hormone-releasing hormone (GHRH) family. Its sequence corresponds to the fully active 44-amino-acid form of human GHRH, with a single structural modification: the addition of a trans-3-hexenoyl group at the N-terminus. That modification is not found in the naturally occurring hormone and was introduced deliberately during development to improve stability against enzymatic degradation. The compound is therefore best described as a stabilized analogue rather than a naturally occurring peptide.
The native hormone is produced in the hypothalamus and acts on the anterior pituitary. Binding of GHRH to its receptor stimulates synthesis and release of growth hormone into circulation. Because the analogue retains the receptor-binding region of the parent sequence, it engages the same receptor and triggers the same downstream signaling. The result is increased growth hormone secretion from pituitary cells, which in turn influences hepatic production of insulin-like growth factor 1. This axis is the basis for the compound's measured biological effects.
Interest in this peptide developed because native GHRH has a short circulating lifetime. The N-terminal modification slows cleavage by dipeptidyl peptidase IV, an enzyme that removes the first two residues of many peptides and terminates their activity. Slower degradation means a longer window of receptor stimulation per administration. This design logic parallels other modified peptide hormones, where a small chemical change at a vulnerable site yields a more durable molecule without altering the core mechanism of action.
The hexenoyl cap slows the enzyme step that trims the amino terminus of native GHRH, the same step that shortens its active lifetime in circulation. As a result, the modified peptide persists longer in plasma than the unmodified hormone in side-by-side comparison. Receptor activity stays broadly comparable, because the added group sits away from the residues that contact the binding site. This combination, preserved receptor activity with reduced degradation, explains why the analog was developed instead of the native sequence.
Several compounds share the GHRH framework, including sermorelin, the shorter 1-29 fragment, and other analogs built on the full 1-44 chain. Naming follows a common convention: a stem that identifies the peptide plus a suffix marking analog status. Reports may describe tesamorelin by its sequence fragment, as a GHRH(1-44) analog, or by its amino-terminal modification. Indexing the compound therefore requires searching all of these forms, since some older literature predates the current international nonproprietary name.
Metabolic interest in this compound centers on fat distribution rather than on hormone levels alone. Imaging trials in adults with excess abdominal fat report reductions in visceral adipose tissue, while subcutaneous depots change comparatively little. Growth hormone and IGF-1 are presumed to carry the effect, but the separate contribution of each is not firmly established. Whether these changes persist after treatment stops, and whether they alter longer-term health outcomes, remain open questions that published work does not answer consistently.
Tesamorelin is a synthetic peptide of forty-four amino acids whose sequence reproduces human growth hormone-releasing hormone. Its distinguishing feature sits at the amino terminus, where a trans-3-hexenoyl group replaces the free amine. That acylation slows cleavage by dipeptidyl peptidase IV, an enzyme that otherwise removes the first two residues and inactivates the natural hormone quickly. The modified peptide therefore persists longer in circulation while keeping the same receptor target. It is handled as a lyophilized solid and dissolved shortly before use.
== Personal life == Collins lives in Roxwell, Chelmsford in a barn conversion which she bought for £1.35 million in 2021. She has described the house as her "dream home" and has had multiple renovations including a swimming pool and a summer house. Collins enjoys gardening and has expressed her love of plants, as well as her passion for animals and nature. She has two dogs and two cats, as well as chickens. Collins has several life-size animal sculptures inside her home and in her garden, including a horse with a disco ball and a giraffe lamp, as well as a wooden Asian mother elephant and its calf, the former of which she donated £22,000 to CoExistence, an environmental art campaign conceptualised by the Elephant Family.
=== Depression === Pindolol has been investigated as an add-on drug to antidepressant therapy with SSRIs like fluoxetine in the treatment of depression since 1994. The rationale behind this strategy has its basis in the fact that pindolol is an antagonist of the serotonin 5-HT1A receptor. Presynaptic and somatodendritic 5-HT1A receptors act as inhibitory autoreceptors, inhibit serotonin release, and are pro-depressive in their action. This is in contrast to postsynaptic 5-HT1A receptors, which mediate antidepressant effects. By blocking 5-HT1A autoreceptors at doses that are selective for them over postsynaptic 5-HT1A receptors, pindolol may be able to disinhibit serotonin release and thereby improve the antidepressant effects of SSRIs and clomipramine. The results of augmentation therapy with pindolol have been encouraging in early studies of low quality. A 2015 systematic review and meta-analysis of five randomized controlled trials found no overall significant benefit at 2.5 mg although, with regard to patients with SSRI-resistant depression, "once-daily high-dose pindolol (7.5 mg qd) appears to show a promising benefit in these patients". On the other hand, a 2017 systematic review indicated that pindolol's efficacy has been demonstrated in high evidence studies. Initiating pharmacotherapy with an SSRI plus pindolol might accelerate the SSRI's therapeutic impact. Pindolol's antidepressive efficacy may predominantly result from its ability to desensitize 5-HT1A autoreceptors.
Elagolix is taken by the oral route of administration, in contrast to other GnRH modulators. The oral bioavailability of elagolix in humans is not described in the Food and Drug Administration (FDA) label for the medication, but in animal research elagolix showed a low oral bioavailability of 5.8% in rats and 11% in monkeys. Following administration, elagolix is rapidly absorbed, with peak concentrations occurring after 0.5 to 1.5 hours. The drug accumulation ratio of elagolix at 150 mg once per day is 0.98 and at 200 mg twice per day is 0.89, indicating that it is not accumulated in the body with continuous administration. At steady state, peak levels of elagolix at 150 mg once per day are 574 ng/mL and at 200 mg twice per day are 774 ng/mL while area-under-the-curve levels of elagolix at 150 mg once per day are 1,292 ng•hour/mL and at 200 mg twice per day are 1,725 ng•hour/mL. A toxicology study found that levels of elagolix in women after a single dose of 1,200 mg were 17 times higher than in women taking 200 mg twice daily. Taking elagolix with a high-fat meal has been found to decrease its peak levels by 36% and its area-under-the-curve levels by 24%. In terms of distribution, the plasma protein binding of elagolix is 80% and its blood-to-plasma ratio is 0.6. The volume of distribution at steady state is 1,674 L at 150 mg once per day and 881 L at 200 mg twice per day. Elagolix is metabolized in the liver, with the major pathway being by CYP3A and minor pathways including by CYP2D6, CYP2C8, and UDP-glucuronosyltransferases.
==== Weight loss ==== Prior to the MERIT study, numerous meta-analyses of studies on ESG report a total body weight loss of approximately 16% at one year. Excess weight loss was observed to be approximately 60% at one year. Weight loss reported from high volume community practices that have both expertise in ESG and robust longitudinal aftercare programs with dietitians have shown even greater outcomes, with total body weight loss approaching 30% and excess weight loss of 66% at one year.
Sources: en.wikipedia.org
The Federal Office for Radiation Protection's monitoring network measures natural radiation exposure through the local dose rate (ODL), expressed in microsieverts per hour (μSv/h). In Germany, the natural ODL ranges from approximately 0.05 to 0.18 μSv/h, depending on local conditions. The ODL monitoring network has been operational since 1973 and currently comprises 1800 fixed, automatically operating measuring points. Its primary function is to provide early warning for the rapid detection of increased radiation from radioactive substances in the air in Germany. Spectroscopic probes have been successfully utilized since 2008 to determine the contribution of artificial radionuclides in addition to the local dose rate, showcasing the network's advanced capabilities. In addition to the ODL monitoring network of the Federal Office for Radiation Protection, there are other federal monitoring networks at the Federal Maritime and Hydrographic Agency and the Federal Institute of Hydrology, which measure gamma radiation in water; the German Meteorological Service measures air activity with aerosol samplers. To monitor nuclear facilities, the relevant federal states operate their own ODL monitoring networks. The data from these monitoring networks are automatically fed into the Integrated Measurement and Information System (IMIS), where they are used to analyze the current situation. Many countries operate their own ODL monitoring networks to protect the public. In Europe, these data are collected and published on the EURDEP platform of the European Atomic Energy Community.
brevicaule complex. DNA analysis however shows that more than 99% of all current varieties of potatoes are direct descendants of a subspecies that once grew in the lowlands of south-central Chile. Most modern potatoes grown in North America arrived through European settlement and not independently from the South American sources. At least one wild potato species, Solanum fendleri, occurs in North America; it is used in breeding for resistance to a nematode species that attacks cultivated potatoes. A secondary center of genetic variability of the potato is Mexico, where important wild species used extensively in modern breeding are found, such as the hexaploid S. demissum, used as a source of resistance to the devastating late blight disease (Phytophthora infestans). Another relative native to this region, Solanum bulbocastanum, has been used to genetically engineer the potato to resist potato blight. Many such wild relatives are useful for breeding resistance to P. infestans. Little of the diversity found in Solanum ancestral and wild relatives is found outside the original South American range. This makes these South American species highly valuable in breeding. The importance of the potato to humanity is recognised in the United Nations International Day of Potato, to be celebrated on 30 May each year, starting in 2024.
In pharmacology, inorganic bromide compounds, especially potassium bromide, were frequently used as general sedatives in the 19th and early 20th century. Porsche in 1828 used KBr for scrofula. Otto Graf in a 1842 thesis reported that he became impotent while taking 1.8 g/day for two weeks as a self-experiment, and recovered sexual function upon ending the intake. Huette in 1850 reported that it caused impotence and loss of libido. Charles Locock in 1856 administered to women with "hysterical epilepsy", whose symptoms included masturbation. Locock theorized that masturbation caused epilepsy in these cases, and adiminstered KBr based on its anaphrodisiac effect. It caused a remission of epilepsy and masturbation. Locock did not understand KBr as an anticonvulsant in its own right. Subsequent research in the 1860s established KBr as generally effective for epilepsy, not just "hysterical" epilepsy, and it came into widespread use. In 1901, the Hospital for the Palsied and Epileptic in London was buying ~2 ton/year of KBr. Bromides also were recommended for insomnia, palpitations, and general neuroses, until barbituates supplanted them around 1930. It remained the only effective anticonvulsant, until the discovery of phenobarbital in 1912. Bromides in the form of simple salts are still used as anticonvulsants in both veterinary and human medicine, although the latter use varies from country to country. For example, the U.S.
=== January 2005 === On 24 January 2005, the ACLU accused the Pentagon of deliberately closing investigations over Human Rights violations and torture cases before they were over. Human Rights Watch accused Iraqi security forces of using torture and improper treatments on prisoners. Arbitrary arrests and long periods of isolation are now common. Human Right Watch interviewed 90 prisoners, among which 72 said they had been tortured during interrogation. Sarah Leah Whitson, HRW director, said that the Iraqi provisional government was not holding to its promise to stand by Human Rights: "A new Iraqi government requires more than a change of leadership - it requires a change of attitude about basic human dignity".
ASR-2001 (2CB-5PrO) is a propoxy TWEETIO and another notable analogue of 2C-B which is under development for treatment of psychiatric disorders. FLY derivatives of 2C-B like 2C-B-FLY, 2C-B-DRAGONFLY, and 2C-B-BUTTERFLY are analogues in which the methoxy groups of 2C-B on the phenyl ring have been cyclized into furan or other rings to form benzodifuran and other tricyclic compounds. 2-OH-2C-B is the 2-O-desmethylated analogue of 2C-B and shows similar potency as a serotonin 5-HT2A receptor agonist in vitro. Cyclized phenethylamine derivatives of 2C-B in which the side chain has been cyclized in some way include DOB-CR (2C-B-CR), 2CB-Ind, 2C-B-5-hemiFLY-α6 (BNAP), 2CB7 (2C-B-5-hemiFLY-β7), TCB-2 (2CBCB), 2C-B-PYR, 2C-B-3PIP, 2C-B-3PIP-NBOMe, 2C-B-3PIP-POMe, 2CBecca, 2CJP, 2CLisaB, ZC-B, 2C-B-aminorex (2C-B-AR), and 2C-B-morpholine (2C-B-MOR), among others. Other related cyclized compounds, while not technically phenethylamines or 2C-B derivatives, include 2C-B-BZP and 2C-B-PP. A notable positional isomer of 2C-B is the scaline and mescaline analogue 4-bromomescaline (4-Br-3,5-DMPEA). Deuterated isotopologues of 2C-B such as 2CB-2OCD3 (2-trideuteromethoxy-2C-B), 2CB-5OCD3 (5-trideuteromethoxy-2C-B), and hexadeutero-2C-B (2,5-di(trideuteromethoxy)-2C-B) among others have been described.
Sources: en.wikipedia.org
It is a laboratory-made peptide of forty-four amino acids whose sequence matches human growth hormone-releasing hormone, with a modified amino terminus. The modification is a short unsaturated fatty acid chain attached to the first residue. This change slows enzymatic breakdown and lengthens the time the peptide stays active in circulation.
The clinical program was designed around HIV-associated lipodystrophy, a condition in which fat accumulates abnormally around the internal organs. Trials enrolled that specific population, so the evidence base covers it rather than the general population. Regulators approved the drug for the studied indication only, and promotion outside it is not permitted.
Growth hormone therapy supplies the finished hormone directly, while this peptide acts upstream and asks the pituitary to secrete its own. That difference means the response depends on a functioning pituitary and on the body's normal feedback loops. It also means the circulating hormone profile is pulsatile rather than a flat, injected level.
特沙莫瑞林是国际非专利名称,指一种经过 N 端修饰的生长激素释放激素类似物。它被归类为合成肽,序列与 GHRH(1-44) 密切相关。该名称不指代任何特定品牌或剂型。