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Structure And Receptor Pharmacology — Quick Reference

By Editorial Desk · published 2026-07-24 · last reviewed 2026-08-01 · Guide

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

Reviewed 2026-08-01. Anything still debated is marked as such rather than presented as settled.

Structure And Receptor Pharmacology

CJC-1295 belongs to a class of synthetic peptides modeled on growth hormone releasing hormone, a forty-four amino acid signal produced by the hypothalamus. The compound is built from the first twenty-nine residues of the natural sequence, with four substitutions introduced at positions 2, 8, 15 and 27. These changes were designed to slow enzymatic breakdown while preserving receptor activation. The result is a peptide that is shorter than native GHRH and considerably more resistant to ordinary clearance pathways in circulation.

Two related forms appear under the CJC-1295 name. The simpler analogue, commonly written as modified GRF(1-29), carries the four substitutions but no additional conjugation. The second form attaches a maleimidopropionic acid linker to a lysine residue, a modification frequently called the drug affinity complex. That linker reacts with the free thiol on serum albumin to form a covalent bond. Because albumin has a long residence time in blood, the conjugated peptide stays in circulation far longer than the unconjugated analogue.

Compound Identity and Development History

CJC-1295 is a synthetic peptide built as a long-acting analogue of growth hormone-releasing hormone. Its backbone matches the first twenty-nine residues of the natural human hormone, with four amino acid substitutions added to slow enzymatic breakdown. A reactive maleimide group, commonly termed the drug affinity complex, allows the peptide to attach to circulating albumin after administration. That albumin attachment keeps the molecule in the bloodstream for an extended period instead of being cleared within minutes.

The compound emerged from work at a Canadian biotechnology firm in the early 2000s. Early human studies examined its effect on growth hormone and insulin-like growth factor 1 in healthy volunteers and in people with HIV-associated fat redistribution. Reports described sustained increases in both markers after a single injection. Development did not advance to regulatory approval, and the clinical programme was later discontinued. The molecule is now encountered mainly as a research chemical rather than a marketed medicine.

Cjc-1295 at a glance

PropertyValueNotes
Peptide classSynthetic GHRH analogueBuilt on a 29 residue sequence
Primary targetGHRH receptor (GHRHR)Class B G protein coupled receptor
Unconjugated half lifeMinutesLimited by protease degradation
Key modificationFour residue substitutionsPositions 2, 8, 15 and 27
Common synonymModified GRF(1-29)Usually denotes the form without DAC

Albumin Binding and Duration of Action

The distinguishing feature of the DAC form is a maleimide-containing group that reacts with the free thiol of cysteine-34 on human serum albumin. This reaction forms a covalent bond without enzymatic assistance, and it takes place after the peptide enters the bloodstream. Because albumin is abundant and long-lived, the attached peptide is carried through circulation far longer than an unmodified fragment would survive. The chemistry is a deliberate pharmacokinetic strategy rather than a change to receptor activity.

Enzymatic protection is a separate mechanism from plasma protein binding. The four substitutions in the backbone reduce recognition by dipeptidyl peptidase IV, which normally cleaves the natural hormone within minutes. Without the reactive group, this resistance still yields only a short window of activity, generally reported in the range of tens of minutes. With it, reported half-lives in early human work extended to several days. The size of that gap is the main practical distinction between the two materials.

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Analytical Measurement And Stability

Identity and purity are established with reversed phase high performance liquid chromatography coupled to mass spectrometry. The chromatographic step separates the target peptide from truncated sequences and deletion products, while the mass measurement confirms the expected molecular weight to within a fraction of a dalton. Because the two common variants differ by the presence of the linker, mass alone can distinguish them in the unconjugated state. Amino acid analysis and peptide mapping are used when sequence level confirmation is required.

Lyophilized material is generally stable for extended periods when held at minus twenty degrees Celsius or below and protected from moisture and light. In solution the peptide is more labile; bond hydrolysis, aggregation and oxidation of susceptible residues all proceed faster at ambient temperature. Repeated freeze and thaw cycles should be avoided because they promote clumping and loss of soluble material. The conjugated variant adds a further consideration, since the maleimide group can hydrolyze in aqueous buffer and lose its ability to react with albumin.

Further detail

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Inflammation of the esophagus is known as esophagitis. Reflux of gastric acids from the stomach, infection, substances ingested (for example, corrosives), some medications (such as bisphosphonates), and food allergies can all lead to esophagitis. Esophageal candidiasis is an infection of the yeast Candida albicans that may occur when a person is immunocompromised. As of 2021 the causes of some forms of esophagitis, such as eosinophilic esophagitis, are not well-characterized, but may include Th2-mediated atopies or genetic factors. There appear to be correlations between eosinophilic esophagitis, asthma (itself with an eosinophilic component), eczema, and allergic rhinitis, though it is not clear whether these conditions contribute to eosinophilic esophagitis or vice versa, or if they are symptoms of mutual underlying factors. Esophagitis can cause painful swallowing and is usually treated by managing the cause of the esophagitis - such as managing reflux or treating infection.

Neuroleptic malignant syndrome (NMS) is a rare but life-threatening reaction that can occur in response to ingesting antipsychotics (neuroleptics) or other drugs that block the effects of dopamine. Symptoms include high fever, confusion, rigid muscles, variable blood-pressure, sweating, and fast heart-rate. Complications may include muscle breakdown (rhabdomyolysis), high blood potassium, kidney failure, or seizures. Any medications within the family of antipsychotics can cause the condition, though typical antipsychotics appear to entail a higher risk than atypicals, specifically first-generation antipsychotics like haloperidol. Onset is often within a few weeks of starting the medication but can occur at any time. Risk factors include dehydration, agitation, and catatonia. Rapidly decreasing the use of levodopa or other dopamine agonists, such as pramipexole, may also trigger the condition. The underlying mechanism involves blockage of dopamine receptors. Diagnosis is based on symptoms. Management includes stopping the triggering medication, rapid cooling, and starting other medications. Medications used include dantrolene, bromocriptine, and diazepam. The risk of death among those affected is about 10%. Rapid diagnosis and treatment is required to improve outcomes. Many people can eventually be restarted on a lower dose of antipsychotic. As of 2011, about 15 per 100,000 (0.015%) patients in psychiatric hospitals on antipsychotics are affected per year. In the second half of the 20th century rates were over 100 times higher at about 2% (2,000 per 100,000).

Sources: en.wikipedia.org

Background from the literature

== Medical uses == Buserelin is approved for the treatment of hormone-responsive cancers including prostate cancer and premenopausal breast cancer, sex hormone-dependent uterine diseases including endometrial hyperplasia, endometriosis, and uterine fibroids, and in assisted reproduction for female infertility. It is also used off-label for the treatment of precocious puberty, as a puberty blocker in transgender children, and as a component of transgender hormone therapy. In ovulation induction, buserelin is used for pituitary suppression as an adjunct to gonadotropin administration. It has also been assessed as a nasal spray for use as a hormonal contraceptive in women, with a 96% anovulation rate.

Before (and, occasionally, after) the discovery of radioactivity, uranium was primarily used in small amounts for yellow glass and pottery glazes, such as uranium glass and in Fiestaware. The discovery and isolation of radium in uranium ore (pitchblende) by Marie Curie sparked the development of uranium mining to extract the radium, which was used to make glow-in-the-dark paints for clock and aircraft dials. This left a prodigious quantity of uranium as a waste product, since it takes three tonnes of uranium to extract one gram of radium. This waste product was diverted to the glazing industry, making uranium glazes very inexpensive and abundant. Besides the pottery glazes, uranium tile glazes accounted for the bulk of the use, including common bathroom and kitchen tiles which can be produced in green, yellow, mauve, black, blue, red and other colors.

Only extensive modelling can enable the exploration of dynamic gene expression in a form suitable for research and design due to the numerous involved species and the intricacy of their relationships. Dynamic simulations of the entire biomolecular interconnection involved in regulation, transport, transcription, induction, and translation enable the molecular level detailing of designs. As opposed to modelling artificial networks a posteriori, this is contrasted.

Sources: en.wikipedia.org

Reference notes

=== Causes === Causes of insufficient vitamin D synthesis in the skin include insufficient exposure to UVB light from sunlight due to living in high latitudes (farther distance from the equator with resultant shorter daylight hours in winter). Serum concentration by the end of winter can be lower by one-third to half that at the end of summer. The prevalence of vitamin D deficiency increases with age due to a decrease in 7-dehydrocholesterol synthesis in the skin and a decline in kidney capacity to convert calcidiol to calcitriol, the latter seen to a greater degree in people with chronic kidney disease. Despite these age effects, elderly people can still synthesize sufficient calcitriol if enough skin is exposed to UVB light. Absent that, a dietary supplement is recommended. Other causes of insufficient synthesis are sunlight being blocked by air pollution, urban/indoor living, long-term hospitalizations and stays in extended care facilities, cultural or religious lifestyle choices that favor sun-blocking clothing, recommendations to use sun-blocking clothing or sunscreen to reduce risk of skin cancer, and lastly, the UV-B blocking nature of dark skin. Consumption of foods that naturally contain vitamin D is rarely sufficient to maintain a recommended serum concentration of 25(OH)D in the absence of the contribution of skin synthesis. Fractional contributions are roughly 20% diet and 80% sunlight.

=== Other cancer causes === The principal risks for penile cancer are HPV, Phimosis and smoking. There is also an association between adult circumcision and an increased risk of invasive penile cancer; this is believed to be from men being circumcised as a treatment for penile cancer or a condition that is a precursor to cancer rather than a consequence of circumcision itself. There is some evidence that circumcision is associated with reduced risk of prostate cancer.

=== Florists' attitudes === Many traditional retail florists have a deep-rooted disdain for modern wire services. This comes from the perception that companies such as FTD, 1800flowers, From You Flowers and Teleflora take floral orders away from the local business and extract excessive commission. FTD was formerly a co-op, owned by its member florists. In 1994 the board of directors made the decision to sell the co-op to Perry Capital. The revenue from the sale was disbursed amongst the member florists, more senior florists being paid substantially more than the more junior florists. At this point FTD became a for-profit company.

Sources: en.wikipedia.org

Frequently asked questions

Is CJC-1295 the same as modified GRF(1-29)?

The names are often used interchangeably in casual writing, but they are not strictly identical. Modified GRF(1-29) refers to the unconjugated analogue carrying only the four substitutions. The version sold as CJC-1295 with DAC includes the albumin binding linker and clears much more slowly.

What does the acronym DAC refer to?

DAC stands for drug affinity complex, a term describing the maleimidopropionic acid linker. This group forms a covalent bond with the cysteine residue on serum albumin after administration. The resulting adduct is what extends the circulating half life from minutes to days.

Does this peptide occur naturally in the body?

No. It is entirely synthetic and does not correspond to any known endogenous peptide. The design starts from human growth hormone releasing hormone and introduces deliberate substitutions. Any biological effect comes from mimicking the natural hormone at its receptor.

What is CJC-1295?

It is a synthetic peptide analogue of growth hormone-releasing hormone. Four substitutions in its sequence make it more resistant to enzymatic degradation than the natural hormone. In the version carrying a drug affinity complex, the peptide binds albumin and remains in circulation for days.

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