Everything below concerns 垂体受体. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.
Updated 2026-06-05. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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 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。
| Property | Value | Notes |
|---|---|---|
| Molecular weight | Approximately 5,136 Da | Based on the 44-amino-acid peptide backbone and N-terminal modification. |
| Appearance | White to off-white lyophilized powder | Usually supplied in single-use vials for reconstitution. |
| Solubility | Freely soluble in water; slightly soluble in some organic solvents | Peptide nature supports aqueous reconstitution. |
| Typical storage | 2–8 °C, protected from light | Refrigeration reduces degradation; avoid freezing unless specified. |
| Common analytical method | Reverse-phase high-performance liquid chromatography | Used for identity, purity, and quantification. |
| Synonyms | Tesamorelin, TH9507, GHRH(1-44) analog | Generic descriptors; avoid proprietary names. |
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.
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Sources: en.wikipedia.org
== Medical uses == Chlorpromazine is used in the treatment of both acute and chronic psychoses, including schizophrenia and the manic phase of bipolar disorder, as well as amphetamine-induced psychosis. Controversially, some psychiatric patients may be given chlorpromazine by force, even if they do not suffer any of the typical conditions the drug is prescribed for. In a 2013 comparison of fifteen antipsychotics in schizophrenia, chlorpromazine demonstrated mild-standard effectiveness. It was 13% more effective than lurasidone and iloperidone, approximately as effective as ziprasidone and asenapine, and 12–16% less effective than haloperidol, quetiapine, and aripiprazole. A 2014 systematic review carried out by Cochrane included 55 trials that compared the effectiveness of chlorpromazine versus placebo for the treatment of schizophrenia. Compared to the placebo group, patients under chlorpromazine experienced less relapse during 6 months to 2 years follow-up. No difference was found between the two groups beyond two years of follow-up. Patients under chlorpromazine showed a global improvement in symptoms and functioning. The systematic review also highlighted the fact that the side effects of the drug were 'severe and debilitating', including sedation, considerable weight gain, a lowering of blood pressure, and an increased risk of acute movement disorders. They also noted that the quality of evidence of the 55 included trials was very low and that 315 trials could not be included in the systematic review due to their poor quality.
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== Methodology == To begin HPTLC, a stationary phase has to be determined to separate different compounds within a mixture. Around 90% of all pharmaceutical separations are performed on normal phase silica gel; however, other stationary phases such as alumina can be used for samples with dissociating compounds and cellulose for ionic compounds. The reverse-phase HPTLC method (similar methodology to reverse-phase TLC) is used for compounds with high polarity. After the selection of the stationary phase, plates are generally washed with methanol and dried in an oven to remove excess solvent. Selection for the mobile phase is one of the most important processes of HPTLC and follows a 'trial and error' pathway. However, the 'PRISMA' system stands as a guideline for finding the optimal mobile phase. The mobile phase is dependent on the absorptivity of the stationary phase and the composition of the compound of interest. The compound is first tested with solutions such as diethyl ether, ethanol, dichloromethane, chloroform for normal phase HPTLC, or solutions such as methanol, acetonitrile, and tetrahydrofuran for reverse phase HPTLC. The retardation factors (Rf) of the compounds with the selected solvent are then analyzed and the solvent that gives the largest Rf is chosen to be the mobile phase for the compound. Then, the mobile solvent strength is tested against hexane (for normal HPTLC) and water (for reverse-phase HPTLC) to determine the need for adjustment.
Sources: en.wikipedia.org
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.
Pivotal trials enrolled adults with HIV and excess visceral abdominal fat, often in the context of antiretroviral therapy. Participants were assessed mainly by computed tomography for visceral adipose tissue. The approved indication remains specific to that population.
Long-term effects on cardiovascular events, mortality, and sustained fat distribution are not well established. Most trials measured changes over months rather than years. Open questions also include whether benefits persist after treatment stops.
tesamorelin 属 GHRH 类似物，作用于垂体受体以促进内源生长激素释放；生长激素本身是直接补充的外源激素。两者在给药逻辑、作用位点和反馈调控路径上并不相同。