This is a working overview of GHRH 类似物, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2025-09-26 and is reviewed periodically as new material appears.
Tesamorelin is a synthetic peptide that acts as an analog of growth hormone-releasing hormone, a natural hypothalamic signal. Its sequence corresponds to the forty-four amino acid form of the human hormone, with a small acyl group attached near the amino terminus. That modification slows enzymatic breakdown and extends the time the peptide remains active in circulation. The compound was developed as a pharmacological way to raise endogenous growth hormone output rather than supplying the hormone directly.
After injection, the peptide binds receptors on somatotroph cells in the anterior pituitary. Receptor activation raises intracellular cyclic AMP and triggers release of stored growth hormone into the bloodstream. Because the compound works through the body's own regulatory system, growth hormone pulses retain much of their normal feedback control. Repeated administration also raises insulin-like growth factor 1, a hormone produced mainly in the liver. Investigators treat that rise as a marker that the pituitary axis has been engaged.
Clinical interest in tesamorelin arose from the need to address visceral adiposity in people living with HIV. Antiretroviral therapy improved survival but was associated in some patients with central fat accumulation, altered lipid profiles, and metabolic complications. This condition, often called HIV-associated lipodystrophy, involves excess visceral adipose tissue that is difficult to manage through diet and exercise alone. Investigators evaluated tesamorelin because GHRH analogs can stimulate growth hormone secretion and influence fat distribution without direct liposuction or invasive procedures.
A Phase 3 program led to regulatory approval in the United States in 2010 for reduction of excess visceral abdominal fat in adults with HIV and lipodystrophy. Subsequent studies examined effects on liver fat, muscle area, and metabolic markers, with mixed findings for some endpoints. Long-term cardiovascular outcomes and effects on mortality remain uncertain because most trials were relatively short and focused on imaging-based fat measurements. Use in populations without HIV has been studied experimentally but is not part of the approved indication.
Tesamorelin is a synthetic analog of growth hormone-releasing hormone, a peptide hormone produced by the hypothalamus. The molecule retains the 44-amino-acid sequence of human GHRH and carries a trans-3-hexenoyl modification at its N-terminus. This modification increases resistance to enzymatic degradation and extends the peptide's functional stability relative to native GHRH. The compound is supplied as a lyophilized powder for reconstitution and subcutaneous administration in clinical settings. Its development code was TH9507, and it belongs to the GHRH analog class. It is not a growth hormone product; instead, it acts upstream to stimulate endogenous growth hormone release.
| Property | Value | Notes |
|---|---|---|
| Drug class | Peptide hormone analog | Acts at the growth hormone-releasing hormone receptor |
| Receptor | Growth hormone-releasing hormone receptor | G protein-coupled; raises cyclic AMP in somatotrophs |
| Key mediator | Insulin-like growth factor 1 | Increases with repeated administration |
| Main studied population | Adults with HIV-associated lipodystrophy | Trials measured visceral adipose tissue by imaging |
| Route | Subcutaneous injection | Given once daily in clinical use |
研究背景集中在特定人群的体成分改变，尤其是与脂肪分布异常相关的内脏脂肪堆积。不同地区对它的监管状态与获批适应症并不一致，部分市场仅限特定诊断人群使用。在一般人群中的长期效应、与其他激素的相互作用以及停药后的维持情况仍属开放问题，现有数据不足以给出普遍结论。
tesamorelin 是一种人工合成的四十四肽，序列与内源性生长激素释放激素（GHRH）的 1-44 片段一致，区别在于 N 端加接了一个反式-3-己烯酰基。该修饰抑制二肽基肽酶 IV 的快速切割，从而延长分子在循环中的存留时间。作为肽类分子，它难以经胃肠道吸收，文献中讨论的均是注射途径。分类上通常把它归为 GHRH 类似物，以区别于生长激素本身。
作用位置在垂体前叶。tesamorelin 与 GHRH 受体结合后激活腺苷酸环化酶，升高细胞内 cAMP，再经蛋白激酶 A 通路促进生长激素的合成与释放。由于它作用于内源调控节点，生长激素仍以脉冲方式分泌，而不是被持续抬升到固定水平。生长激素随后在肝脏等组织诱导胰岛素样生长因子 1 产生，构成完整的生长激素轴响应。
The new tools of molecular biology changed the study of bird systematics, which changed from being based on phenotype to the underlying genotype. The use of techniques such as DNA–DNA hybridization to study evolutionary relationships was pioneered by Charles Sibley and Jon Edward Ahlquist, resulting in what is called the Sibley–Ahlquist taxonomy. These early techniques have been replaced by newer ones based on mitochondrial DNA sequences and molecular phylogenetics approaches that make use of computational procedures for sequence alignment, construction of phylogenetic trees, and calibration of molecular clocks to infer evolutionary relationships. Molecular techniques are also widely used in studies of avian population biology and ecology.
The major long-term complications of diabetes relate to damage to blood vessels at both macrovascular and microvascular levels. Diabetes doubles the risk of cardiovascular disease, and about 75% of deaths in people with diabetes are due to coronary artery disease. Other macrovascular morbidities include stroke and peripheral artery disease. Microvascular disease affects the eyes, kidneys, and nerves. Damage to the retina, known as diabetic retinopathy, is the most common cause of blindness in people of working age. The eyes can also be affected in other ways, including development of cataract and glaucoma. It is recommended that people with diabetes visit an optometrist or ophthalmologist once a year. Diabetic nephropathy is a major cause of chronic kidney disease, accounting for over 50% of patients on dialysis in the United States. Diabetic neuropathy, damage to nerves, manifests in various ways, including sensory loss, neuropathic pain, and autonomic dysfunction (such as postural hypotension, diarrhea, and erectile dysfunction). Loss of pain sensation predisposes to trauma that can lead to diabetic foot problems (such as ulceration), the most common cause of non-traumatic lower-limb amputation. Hearing loss is another long-term complication associated with diabetes. Based on extensive data and numerous cases of gallstone disease, it appears that a causal link might exist between type 2 diabetes and gallstones. People with diabetes are at a higher risk of developing gallstones compared to those without diabetes.
Gonadotropin-releasing factor (GnRF, GRF); Gonadotropin-releasing hormone (GnRH, GRH) Follicle-stimulating hormone-releasing factor (FRF, FSH-RF); Follicle-stimulating hormone-releasing hormone (FRH, FSH-RH) Luteinizing hormone-releasing factor (LRF, LHRF); Luteinizing hormone-releasing hormone (LRH, LHRH) Follicle-stimulating hormone and luteinizing hormone–releasing factor (FSH/LH-RF); Follicle-stimulating hormone and luteinizing hormone-releasing hormone (FSH/LH-RH) Luteinizing hormone and follicle-stimulating hormone–releasing factor (LH/FSH-RF); Luteinizing hormone and follicle-stimulating hormone-releasing hormone (LH/FSH-RH) Gonadorelin (INN for pharmaceutical form) Gonadoliberin
=== Pharmacokinetics === In the field of pharmacokinetics, steady state refers to the condition in which the rate of drug administration is balanced by the rate of drug elimination, resulting in a stable concentration of the drug in the bloodstream over time. This equilibrium typically occurs following repeated dosing or continuous infusion, and is used to ensure consistent therapeutic drug levels. For most drugs exhibiting first-order kinetics, steady state is generally achieved after approximately four to five half-lives, at which point the changes in plasma concentrations between doses become minimal and predictable. At steady state, drug concentrations do not remain at a single, unchanging value but rather fluctuate within a limited range bounded by peak (Cmax) and trough (Cmin) values across each dosing interval. Ideally, this range is maintained above the minimum effective (therapeutic) concentration and below the threshold for adverse effects, thereby achieving concentrations within the so-called therapeutic window.
Sources: en.wikipedia.org
==== Other activities ==== In addition to the opioid receptors, naltrexone binds to and acts as an antagonist of the opioid growth factor receptor (OGFR) and toll-like receptor 4 (TLR4). It has been proposed that low doses of naltrexone (1 to 5 mg/day) produce TLR4 antagonism, and standard clinical doses (50 to 100 mg/day) exert opioid receptor and OGFR antagonism. The interactions of naltrexone with TLR4 are claimed to be involved in the therapeutic effects of low-dose naltrexone.
lisdexamphetamine is the International Nonproprietary Name (INN) and is a contraction of L-lysine-dextroamphetamine. As of November 2020, lisdexamphetamine is sold under the following brand names: Aduvanz, Elvanse, Juneve, Samexid, Tyvense, Venvanse, and Vyvanse.
The maximum life span of transgenic mice has been extended about 20% by overexpression of human catalase targeted to mitochondria A comparison of 7 non-primate mammals (mouse, hamster, rat, guinea-pig, rabbit, pig and cow) showed that the rate of mitochondrial superoxide and hydrogen peroxide production in heart and kidney were inversely correlated with maximum life span A study of 8 non-primate mammals showed an inverse correlation between maximum life span and oxidative damage to mtDNA (mitochondrial DNA) in heart & brain A study of several species of mammals and a bird (pigeon) indicated a linear relationship between oxidative damage to protein and maximum life span There is a direct correlation between DNA repair and maximum life span for mammalian species Drosophila (fruit-flies) bred for 15 generations by only using eggs that were laid toward the end of reproductive life achieved maximum life spans 30% greater than that of controls Overexpression of the enzyme which synthesizes glutathione in long-lived transgenic Drosophila (fruit-flies) extended maximum lifespan by nearly 50% A mutation in the age−1 gene of the nematode worm Caenorhabditis elegans increased mean life span 65% and maximum life span 110%. However, the degree of lifespan extension in relative terms by both the age-1 and daf-2 mutations is strongly dependent on ambient temperature, with ≈10% extension at 16 °C and 65% extension at 27 °C. Fat-specific Insulin Receptor KnockOut (FIRKO) mice have reduced fat mass, normal calorie intake and an increased maximum life span of 18%.
=== Histology === Histological structure of type 1 consists of tight tissue fibers and loose connective tissues. The surrounding loose fibers are rich in blood vessels with pathways for nerves. Tendinous fibers are rarely found and are in single direction. Type 2 juncturae tendinum is also composed of single direction fibers like type 1, but with thicker bundles. Histological structure of the type 3 juncturae is denser and thicker than type 2 juncturae and tendinous fibers are arranged in two layers. Tendinous fibers of the type 3 show crosswise direction with single direction and oblique bundles. No muscular tissue is observed in any type of the juncturae tendinum.
In March 2018 Sara Rojas and her team published their research on drug incorporation and delivery with various biocompatible MOFs other than CD-MOF-1 through simulated cutaneous administration. The group studied the loading and release of ibuprofen (hydrophobic) and aspirin (hydrophilic) in three biocompatible MOFs (MIL-100(Fe), UiO-66(Zr), and MIL-127(Fe)). Under simulated cutaneous conditions (aqueous media at 37 °C) the six different combinations of drug-loaded MOFs fulfilled "the requirements to be used as topical drug delivery systems, such as released payload between 1 and 7 days" and delivering a therapeutic concentration of the drug of choice without causing unwanted side effects. The group discovered that the drug uptake is "governed by the hydrophilic/hydrophobic balance between cargo and matrix" and "the accessibility of the drug through the framework". The "controlled release under cutaneous conditions follows different kinetics profiles depending on: (i) the structure of the framework, with either a fast delivery from the open structure MIL-100 or a slower drug release from the narrow 1D pore system of MIL-127 or (ii) the hydrophobic/hydrophilic nature of the cargo, with a fast (Aspirin) and slow (Ibuprofen) release from the UiO-66 matrix." Moreover, a simple ball milling technique is used to efficiently encapsulate the model drugs 5-fluorouracil, caffeine, para-aminobenzoic acid, and benzocaine. Both computational and experimental studies confirm the suitability of [Zn4O(dmcapz)3] to incorporate high loadings of the studied bioactive molecules.
Sources: en.wikipedia.org
Common aqueous acids include hydrochloric acid (a solution of hydrogen chloride that is found in gastric acid in the stomach and activates digestive enzymes), acetic acid (vinegar is a dilute aqueous solution of this liquid), sulfuric acid (used in car batteries), and citric acid (found in citrus fruits). As these examples show, acids (in the colloquial sense) can be solutions or pure substances, and can be derived from acids (in the strict sense) that are solids, liquids, or gases. Strong acids and some concentrated weak acids are corrosive, but there are exceptions such as carboranes and boric acid. The second category of acids are Lewis acids, which form a covalent bond with an electron pair. An example is boron trifluoride (BF3), whose boron atom has a vacant orbital that can form a covalent bond by sharing a lone pair of electrons on an atom in a base, for example the nitrogen atom in ammonia (NH3). Lewis considered this as a generalization of the Brønsted definition, so that an acid is a chemical species that accepts electron pairs either directly or by releasing protons (H+) into the solution, which then accept electron pairs. Hydrogen chloride, acetic acid, and most other Brønsted–Lowry acids cannot form a covalent bond with an electron pair, however, and are therefore not Lewis acids. Conversely, many Lewis acids are not Arrhenius or Brønsted–Lowry acids. In modern terminology, an acid is implicitly a Brønsted acid and not a Lewis acid, since chemists almost always refer to a Lewis acid explicitly as such.
=== Gas chromatography === When IMS is coupled with gas chromatography, common sample introduction is with the GC capillary column directly connected to the IMS setup, with molecules ionized as they elute from GC. A similar technique is commonly used for HPLC. A novel design for corona discharge ionization ion mobility spectrometry (CD–IMS) as a detector after capillary gas chromatography has been produced in 2012. In this design, a hollow needle was used for corona discharge creation and the effluent was entered into the ionization region on the upstream side of the corona source. In addition to the practical conveniences in coupling the capillary to IMS cell, this direct axial interfacing helps us to achieve a more efficient ionization, resulting in higher sensitivity. When used with GC, a differential mobility analyzer is often called a differential mobility detector (DMD). A DMD is often a type of microelectromechanical system, radio frequency modulated ion mobility spectrometry (MEMS RF-IMS) device. Though small, it can fit into portable units, such as transferable gas chromatographs or drug/explosives sensors. For instance, it was incorporated by Varian in its CP-4900 DMD MicroGC, and by Thermo Fisher in its EGIS Defender system, designed to detect narcotics and explosives in transportation or other security applications.
=== Booster preparations === The Atlas booster used for MA-9 sported several technical improvements, most notably an enhanced propulsion system with a hypergolic igniter that would eliminate the need for hold-down time at launch to prevent rough combustion. With seven successful Mercury launches in a row, the failures of the early days seemed like a distant memory by early 1963 and NASA officials had a high degree of confidence in the Atlas that overshadowed its still spotty launch record. At the first meeting of senior MSFC officials for the year (January 11), Walter Williams noted that the Air Force had yet to provide an explanation for two Atlas F failures during the second half of 1962. Until the investigation committees released their findings and cleared the Atlas D of guilt by association, Cooper's flight could be delayed. During the seven months between Schirra's and Cooper's flights, there were five failures of Atlas D vehicles (one of them an Atlas-Agena, the rest operational ICBM tests). NASA did not let its guard down on the Atlas, despite the recent high degree of success enjoyed by Project Mercury. When Atlas 130D received its factory rollout on January 30, it was found to have damaged wiring and had to be sent back for repairs. At his first press conference on February 8, Gordon Cooper admitted to not knowing much about the booster problems and focused instead on the enhancements made to his Mercury capsule.
== Complications == Chronic hyperglycemia over a period of years can produce serious complications including kidney damage, neurological damage, cardiovascular damage, damage to the retina, damage to feet and legs, diabetic neuropathy, impairment of growth and susceptibility to certain infections. Acute severe hyperglycemia is a medical emergency and can rapidly produce serious complications (such as fluid loss through osmotic diuresis). It is most often seen in persons who have uncontrolled insulin-dependent diabetes.
== Structure == Monomeric actin, or G-actin, has a globular structure consisting of two lobes separated by a deep cleft. The bottom of the cleft represents the "ATPase fold", a structure conserved among ATP and GTP-binding proteins that binds to a magnesium ion and a molecule of ATP. Binding of ATP or ADP is required to stabilize each actin monomer; without one of these molecules bound, actin quickly becomes denatured. The X-ray crystallography model of actin that was produced by Kabsch from the striated muscle tissue of rabbits is the most commonly used in structural studies as it was the first to be purified. The G-actin crystallized by Kabsch is approximately 67 x 40 x 37 Å in size, has a molecular mass of 41,785 Da and an estimated isoelectric point of 4.8. Its net charge at pH = 7 is -7.
Sources: en.wikipedia.org
It is a laboratory-made peptide that mimics growth hormone-releasing hormone. It prompts the pituitary gland to release growth hormone and has been studied mainly in adults with HIV-associated lipodystrophy.
Administered growth hormone supplies the hormone directly, while this peptide acts upstream by prompting the pituitary to release it. The indirect route preserves pulsatile secretion and some endogenous feedback, which changes the hormone and IGF-1 profile observed after treatment.
Reductions in visceral adipose tissue appear consistently in randomized trials of the approved population. Effects on peripheral fat, cardiovascular outcomes, and use outside that population are less well established.
It is a synthetic peptide analog of human growth hormone-releasing hormone. It is used clinically to reduce excess visceral abdominal fat in adults with HIV-associated lipodystrophy. It works by stimulating pituitary growth hormone release.