Epithalon 20mg/50mg

Cerebrolysin 2mg, 5mg $60.00 – $110.00

https://gsrs.ncats.nih.gov/ginas/app/beta/substances/37KZM6S21G%20

2mg 5mg

Cerebrolysin is a porcine-derived peptide preparation, with a low molecular mass and a variety of research applications. An interesting thing about cerebrolysin is that its preparation contains nerve growth factors, BDFN (brain derived neurotrophic factor), Ciliary nerve growth factor, p-21 and orexin. This means that cerebrolysin contains molecules with:

Pharmacodynamic properties – it expresses biochemical, physiological and molecular effects within the body.
Neurotrophic properties – it aids in growing, repair and neuron maintenance
Neuroprotective properties – it strengthens the neural pathways as well as the neurons themselves and improves synaptic plasticity.

Cerebrolysin Chemical Structure

It’s a bit difficult talking about cerebrolysin as it does not have a single chemical structure, rather, it’s a combination of several different peptides. As such, cerebrolysin is actually labeled an “orphan drug” by the FDA. What this means is it did show promise in disease treatment and prevention (in clinical trials), but only in orphan diseases. Orphan disease is one that affects fewer than 200,000 people in the US. This is why this peptide mix is not a profitable venture for further, independent studies, and research is only possible with financial help from the government.

But in the particular case of cerebrolysin, the government did, in fact, intervene, due to its potential in dealing with dementia and because of its neuroprotective capabilities.

This peptide mix was first developed in Austria, back in 1940 and has since become a vital medicine in Asia, especially Russia and China. Research studies showed that it has the ability to cross the blood-brain barrier and express its pharmacodynamic effects on both brain and the spinal cord.

But, what does it do?

Since cerebrolysin is not a single chemical compound, as we already said, we can look at it, and its effects, through the components its made of:

Brain-Derived Neurotrophic Factor (BDNF) – this is a protein found in our central nervous system, shown to have a profound effect on neuron growth, synapse growth and health. Research in depression and Alcheimer’s disease revealed disrupted BDNF pattern expression.
Glial Cell Line-Derived Neurotrophic Factor (GCNF) – this is an exceptionally important, naturally occurring peptide that promotes neuron survival, decreases the loss of neurons and, as some studies have pointed out, has the potential to aid the prevention of Parkinson’s and ALS.
Ciliary Neurotrophic Factor (CNTF) – this is an interesting hormone affecting the growth of certain neural cells and has been a subject of numerous trials aimed at treating ALS.
Nerve Growth Factor (NGF) – this is a particularly important peptide which regulates the growth, survival and neuron increase in number. Some studies showed NGF is one of the important factors in programmed cell death and regulation of certain immune system mechanisms.

Looking at these effects, it’s not hard to imagine why scientists used these molecules – to try and merge all these positive effects into one single mix. But were they successful? We actually have some clinical trials atesting to these possibilities:

Cerebrolysin and Dementia – a study done in 2012 evaluated the outcomes of cerebrolysin therapy in patients with Alcheimer’s over the course of a 12 week treatment period. The study showed significant improvements in cognitive functions and the symptoms of dementia lasting up to several months after the study was finished.
Cerebrolysin and Parkinson’s – we know that the onset of Parkinson’s disease has to do with the protection of dopamine producing neurons. The loss of these neurons is what leads to motor deficits characteristic for this disease. Unfortunately, we haven’t had human trials, but the one on mice showed that cerebrolysin administration protected these neurons and also lowered certain hormones responsible for Parkinson’s disease worsening.
Stroke and Brain Injuries – though we don’t have many studies dealing with this topic, some small-scale ones showed cerebrolysin as being not only safe to use, but also helpful in recovery rate if given within 72 hours. Research in infants with brain injury induced communication delay also showed cerebrolysin improved therapeutic outcomes.

Even though these positive effects may seem overwhelming, leaving you wondering why cerebrolysin is not a mainstream, FDA-approved drug still, it’s important to note most of these findings were done on a limited sample (and mostly on animal studies). We have yet to see its effects in large-scale studies and, more importantly, see the long-term benefits of cerebrolysin therapy. Even though the initial results seem promising, we need to be patient and wait for more information before the final verdict.

References:

Allegri RF, Guekht A. Cerebrolysin improves symptoms and delays progression in patients with Alzheimer’s disease and vascular dementia. Drugs Today (Barc). 2012 Apr;48 Suppl A:25-41. doi: 10.1358/dot.2012.48(Suppl.A).1739721. PMID: 22514793.

Plosker GL, Gauthier S. Cerebrolysin: a review of its use in dementia. Drugs Aging. 2009;26(11):893-915. doi: 10.2165/11203320-000000000-00000. PMID: 19848437.

Masliah E, Armasolo F, Veinbergs I, Mallory M, Samuel W. Cerebrolysin ameliorates performance deficits, and neuronal damage in apolipoprotein E-deficient mice. Pharmacol Biochem Behav. 1999 Feb;62(2):239-45. doi: 10.1016/s0091-3057(98)00144-0. PMID: 9972690.

Ozkizilcik A, Sharma A, Lafuente JV, Muresanu DF, Castellani RJ, Nozari A, Tian ZR, Mössler H, Sharma HS. Nanodelivery of cerebrolysin reduces pathophysiology of Parkinson’s disease. Prog Brain Res. 2019;245:201-246. doi: 10.1016/bs.pbr.2019.03.014. Epub 2019 Apr 2. PMID: 30961868.

Hassanein SM, Deifalla SM, El-Houssinie M, Mokbel SA. Safety and Efficacy of Cerebrolysin in Infants with Communication Defects due to Severe Perinatal Brain Insult: A Randomized Controlled Clinical Trial. J Clin Neurol. 2016 Jan;12(1):79-84. doi: 10.3988/jcn.2016.12.1.79. Epub 2015 Sep 11. PMID: 26365023; PMCID: PMC4712290.

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Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse

CJC-1295 DAC $110.00

If you’re a peptide researcher (or plan on becoming one), you should know the difference between CJC-1295 and CJC-1295 DAC. CJC-1295 DAC features an additional component at the end of the peptide chain, also known as a drug affinity complex or DAC.

This small fragment changes the peptide’s functionality and extends its half-life to six to eight days. It might have a prolonged effect of up to two weeks.

Below, we will showcase the main similarities and differences between these two peptides, including their properties, characteristics, and mechanism of action.

What is CJC-1295 DAC peptide?

This peptide resembles the regular CJC-1925 since it is a modified form of natural GHGR (1-29). However, this one differs from CJC-1925. It has an additional molecule known as a “drug affinity complex.”

DAC features a couple of oxygen and nitrogen atoms connected by chemical bonds. According to some findings, this small number of atoms could significantly impact peptide breakdown rate and its use in the body.

What is CJC-1295 Peptide?

This peptide is also known as “modified growth hormone releasing factor (1-29)”, “ModGRF 1-29”, or “Modified GRF (1-29).” You may also encounter the name “CJC-1295, without DAC.”

All these names imply a specific peptide molecule containing a short amino acid chain. As many studies have indicated, this peptide may boost growth hormones in the bloodstream.

Growth hormone may have a significant role in several vital internal activities. It could facilitate cellular reproduction, repair, and growth, help with tissue repair, improve muscle cell development, support skin cells, and other functions.

While the body naturally produces growth hormone, this production tends to naturally decrease. According to some research done in laboratory settings, CJC-1295 may encourage the natural production of growth hormone, increasing its levels, which could lead to quicker repair, fat cell burn, and muscle cell growth.

Differences between CJC-1295 DAC and CJC-1295

As research studies have outlined, here are some fundamental differences between these two peptides.

Half-life

The main distinction lies in their half-lives. CJC-1295 is thought to mimic the body’s natural peptide. The endogenous GHRH has a short half-life of just a couple of minutes. Similarly, CJC-1295 has a brief half-life of around half an hour.

Regarding the second peptide, the additional DAC could significantly alter the organism’s peptide use. Researchers believe that DAC offers a peptide, a lysine linker, which could protect and prevent it from degrading.

Moreover, the DAC component could extend the half-life of this peptide to about six to eight days.

Properties of CJC-1295 DAC peptide

It is believed that CJC-1295 DAC boosts growth hormone levels in the bloodstream. Additionally, several studies suggest the following:

Scientists and researchers need to focus their attention to studying the potential of growth hormones on growth and muscle recovery.
Growth hormone may help convert fatty tissue into energy.
Growth hormones are linked with collagen production in the skin, which means this peptide may also help with skin regeneration and skin cell development.
CJC-1295 DAC may positively impact sleep patterns.
Growth hormone is essential for tissue regeneration and helps the organism recover from damage.

References:

Teichman SL, Neale A, Lawrence B, Gagnon C, Castaigne JP, Frohman LA. Prolonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults. J Clin Endocrinol Metab. 2006 Mar;91(3):799-805. doi: 10.1210/jc.2005-1536. Epub 2005 Dec 13. PMID: 16352683.

Sam L. Teichman, Ann Neale, Betty Lawrence, Catherine Gagnon, Jean-Paul Castaigne, Lawrence A. Frohman, Prolonged Stimulation of Growth Hormone (GH) and Insulin-Like Growth Factor I Secretion by CJC-1295, a Long-Acting Analog of GH-Releasing Hormone, in Healthy Adults, The Journal of Clinical Endocrinology & Metabolism, Volume 91, Issue 3, 1 March 2006, Pages 799–805,

Maria Alba, Danilo Fintini, Alessia Sagazio, Betty Lawrence, Jean-Paul Castaigne, Lawrence A. Frohman, and Roberto Salvatori
American Journal of Physiology-Endocrinology and Metabolism 2006 291:6, E1290-E1294

Alba M, Fintini D, Sagazio A, Lawrence B, Castaigne JP, Frohman LA, Salvatori R. Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse. Am J Physiol Endocrinol Metab. 2006 Dec;291(6):E1290-4. doi: 10.1152/ajpendo.00201.2006. Epub 2006 Jul 5. PMID: 16822960.

Alba, Maria & Fintini, Danilo & Sagazio, Alessia & Lawrence, Betty & Castaigne, Jean-Paul & Frohman, Lawrence & Salvatori, Roberto. (2007). Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse. American journal of physiology. Endocrinology and metabolism. 291. E1290-4. 10.1152/ajpendo.00201.2006.

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MOTS-C 10mg $110.00

Aging happens when cells within the body produce less energy and don’t function properly. The main part of the cell, mitochondria, is responsible for producing cellular energy. It also communicates with the cell’s nucleus, enabling the cell to function properly.

This communication happens through amino acid chains called MDPs or mitochondrially derived peptides. MDPs turn various functions on and off. The symptoms of aging seem to be related to genetic messaging. At the moment, scientists are working to identify each MDP. They have successfully identified one that appears to have multiple benefits when it comes to aging, called MOTS-c.

What is MOTS-c?

This peptide is made from 16 amino acids that manage communication between the nucleus of each cell and mitochondria. Some clinical trials suggest that MOTS-c may positively affect health and well-being, regulating how cells produce energy and control cellular function.

Benefits of MOTS-C

According to some test trials conducted in laboratory settings, scientists concluded the following benefits. However, more research is necessary to support these claims.

Improved Metabolism

Animal studies indicate that MOTS-c improves both glucose metabolism and insulin sensitivity. Therefore, this peptide could be a potential treatment for age-related metabolic conditions, like type 2 diabetes.

Mitochondrial Performance

Numerous age-related conditions and illnesses are linked to minimized mitochondrial function. However, this peptide optimizes mitochondrial function and might help reduce the incidence of disease and cellular damage.

Muscle Strength

As they age, people tend to lose muscle mass, leading to loss of balance, strength, and mobility. Studies conducted on animals indicate that MOTS-c could promote muscle endurance and muscle mass growth.

Stress Resilience

In response to stress, our body releases hormones such as adrenaline and cortisol. These hormones boost blood pressure and heart rates to help your body cope with whatever is causing stress. For the most part, this could be advantageous on a short-term basis.

However, if you expose your body to chronic stress for weeks, months, and years, it could lead to high blood pressure, type 2 diabetes, heart disease, and other stress-related illnesses. MOTS-c could help cells adapt to stressors, which in return may slow down cellular aging.

DNA Repair

Damaged DNA contributes to the aging process. In many studies, MOTS-c has been shown to support DNA repair. It may also positively affect autophagy, the process in which cells remove components that are no longer working or are damaged.

References:

Zheng Y, Wei Z, Wang T. MOTS-c: A promising mitochondrial-derived peptide for therapeutic exploitation. Front Endocrinol (Lausanne). 2023 Jan 25;14:1120533. doi: 10.3389/fendo.2023.1120533. PMID: 36761202; PMCID: PMC9905433.

Wan, W., Zhang, L., Lin, Y. et al. Mitochondria-derived peptide MOTS-c: effects and mechanisms related to stress, metabolism and aging. J Transl Med 21, 36 (2023). https://doi.org/10.1186/s12967-023-03885-2

Reynolds, J.C., Lai, R.W., Woodhead, J.S.T. et al. MOTS-c is an exercise-induced mitochondrial-encoded regulator of age-dependent physical decline and muscle homeostasis. Nat Commun 12, 470 (2021). https://doi.org/10.1038/s41467-020-20790-0

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https://www.peptidesciences.com/melanotan-2-10mg?queryID=21fe0d5a93fd5eab13f77dfcf49032bf&objectID=8&indexName=psm2_default_products

Melanotan 2 $55.00

Melanotan 2 is a synthetic version of human alpha-melanocyte stimulating hormone and acts as a non selective melanocortin-receptor agonist. It was mainly developed as a sunless tanning option, but some clinical studies showed it also causes spontaneous penile erections, as well as general sexual stimulation.

Some of the other “side effects” researchers noticed were reduction in compulsive behavior, reduced glucagon production, hunger suppression and even some limited addiction control.

Melanotan 2 Effects On Autism

There is some additional recent clinical research suggesting there might be a link between Mealnotan 2 and autism. Of course, melanotan treatment cannot reverse autism, sadly, but it may act on some aspects of this disorder and make it more manageable.

In mouse model studies researchers recorded that MT2 stimulated oxytocin release, which had the potential to reduce (in some cases counteract) common ASD behaviors – behaviors that include:

Hand clapping
Bouncing on toes
Body rocking
Holding body parts in unusual positions
Repeating vocalizations etc.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7930850/

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Kisspeptin 5mg/10mg $60.00 – $110.00

Metastin or Kisspeptin is believed to have the ability to prevent the spread of cancer or metastasis. This peptide is produced by the hypothalamus, which stimulates the release of GnRH or gonadotropin-releasing hormone, which then causes follicle-stimulating hormone and luteinizing hormone to be released from the purity gland.

Kisspeptin is used in testosterone replacement therapy instead of hCG to increase testosterone levels. That’s why it has emerged as a crucial regulator of the mammalian reproductive axis.

This peptide was first discovered in 1996 when it managed to inhibit melanoma cell lines. It belongs to a family of peptides that are derived from the KISS1/kiss1 gene structure, forming from prepro-kisspeptin, which has differential proteolysis for a common precursor.

Kisspeptin is classified as an RF or neuroactive peptide with a specific Arg-Phe-NH2 motif.

Benefits:

Kisspeptin binds to receptors in the pituitary gland, triggering a response that prompts the gland to release neurotransmitters, signaling the release of LH and FSH.

Based on numerous animal studies, scientists have managed to uncover the following benefits:

Boosts the production of testosterone naturally
Regulates fertility
Increases sexual drive
Improves immune response
Boosts brain function
Promotes weight loss

How does Kisspeptin work?

This peptide stimulates the release of GnRH or gonadotropin-releasing hormone. It enters the purity gland through receptor sites, causing a gland to release neurotransmitters, which later signal the releases of FH and LH. These hormones play a crucial role in the production of oestradiol and testosterone.

Kisspeptin mimics the action of hCG and clomiphene, and according to some animal studies, it can affect fertility in female and male animals.

Distribution of Kisspeptin

Kisspeptin was first found in the placenta, and later, it has been observed in the small intestine, pancreas, ovaries, and testis in mammals. The primary expression of Kisspeptin and its receptors have been shown in two big neuronal populations within the hypothalamus of rodents, the anteroventral periventricular nucleus and the arcuate nucleus.

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https://www.sciencedirect.com/science/article/pii/S0306453013002369

Oxytocin 10mg $50.00

Oxytocin, also known as the love hormone, helps us bond with our loved ones and is often released through touch, exercise, and music.

What is Oxytocin?

This natural hormone manages crucial aspects of male and female reproductive systems, including lactation, labor, delivery, and certain aspects of human behavior. The hypothalamus produces oxytocin, but the posterior pituitary gland releases and stores this hormone into the bloodstream.

Hormones are chemicals that manage various functions in the human body by carrying messages through blood to tissues, muscles, and organs. These signals instruct your body what to do and when to do it.

The hypothalamus is part of the brain that controls functions such as heart rate, digestion, body temperature, and blood pressure. On the other hand, the pituitary gland is a small, pea-sized endocrine gland placed at the base of the brain, below the hypothalamus.

Synthetic Forms of Oxytocin

A synthetic form of oxytocin is used in hospital settings, particularly when doctors need to induce labor in childbirth if it hasn’t begun naturally or to help with contractions. Healthcare providers may also use this hormone to speed up the delivery of the placenta, which is the third stage of labor, and minimize the risk of heavy bleeding.

Function of Oxytocin

As previously mentioned, the two main functions of oxytocin are to encourage uterine contractions in childbirth and labor and to boost contractions of breast tissue to help with lactation after childbirth.

However, apart from these, oxytocin has other important roles, such as:

Placenta-infant bonding
Romantic attachment
Trust
Recognition
Sexual arousal

The effects of oxytocin on the human brain are complex, and scientists are currently researching the role of oxytocin in various conditions.

PTSD
Depression
Autism spectrum disorder
Anxiety
Anorexia
Addiction

Florea T, Palimariciuc M, Cristofor AC, Dobrin I, Chiriță R, Bîrsan M, Dobrin RP, Pădurariu M. Oxytocin: Narrative Expert Review of Current Perspectives on the Relationship with Other Neurotransmitters and the Impact on the Main Psychiatric Disorders. Medicina (Kaunas). 2022 Jul 11;58(7):923. doi: 10.3390/medicina58070923. PMID: 35888641; PMCID: PMC9318841.

Kendrick KM, Guastella AJ, Becker B. Overview of Human Oxytocin Research. Curr Top Behav Neurosci. 2018;35:321-348. doi: 10.1007/7854_2017_19. PMID: 28864976.

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https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7973386/

NAD+ $55.00

Nicotinamide adenine dinucleotide (NAD+) is a critical coenzyme that’s present in every living cell and, as such, is involved in a number of metabolic and cellular processes. This is why NAD+ is so interesting for many different areas of research such as:

Anti aging
Metabolic disorders
Neurodegenerative disorders
And even cancer research

PeptideShop.com sells NAD+ peptide in vials of 100mg and is meant for laboratory use only. Researchers commonly use it to test its effectiveness on:

DNA damage repair and gene expression
Stress response regulation
Slowing down the progression of degenerative disorders
Metabolism pathway testing

But, as previously mentioned, we are still waiting on large scale human tests.

NAD+ Role In Cellular Maintenance

Cellular NAD exists in two forms:

NAD+
NADH

When there’s a shift in NAD+ and its level drops in favor of NADH, this is a hallmark of aging; though the exact mechanisms that lead to this drop still remain unknown.

Naturally, numerous clinical studies showed that increasing NAD+ levels leads to the reduction of age-related immune and metabolic changes. Meaning there is potential of using NAD+ in treating age related disorders.

NAD+ And Neurodegenerative Disorders

When speaking about aging, one of the most contributing factors is mitochondrial dysfunction in neurons. Aging also speeds up the progression of neurodegenerative disorders, triggering DNA damage and mitochondrial impairment.

Luckily, studies have shown that NAD+ treatment (and even supplementation) helped restore mitochondrial function, enhance neural function and even improve cognitive abilities.

NAD+ And Metabolic Disorders

We’ve seen a dramatic increase in metabolic disorders lately, making it one of the major global health problems. Of course, we use the term metabolic disorders to cluster a whole host of problems such as obesity, diabetes, hypertension, as well as some cardiovascular pathologies.

NAD+ levels directly influence nutrient status in cells, so regulating them stands as a clear guideline to future research in hope of making NAD+ an FDA-approved way of treating metabolic and age related disorders.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7963035/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9512238/

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https://www.sciencedirect.com/science/article/abs/pii/0304416582900332

hGH Fragment 176-191 $80.00

Numerous studies have shown that this peptide may represent numerous opportunities for competent scientists to investigate, especially cartilage regeneration and fatty tissue mitigation.

What is Fragment 176-191 peptide?

This synthetic amino acid sequence mimics the hGH sequence, starting from position 177 to position 191.

AOD 9604, or “lipolytic extract,” is another name for Fragment 176-191. Many researchers argue that Fragment 177-191 may be an important research compound in the context of obesity. They believe it can potentially burn fat in animal models in laboratory settings.

Despite positive results, Fragment 176-191 hasn’t been used for human research purposes and doesn’t have official medical approvals.

Growth hormone

According to research, it appears that hGH Fragment 176-191 may not produce any side effects often related to hGH supplementation. Several adverse effects, such as, impaired glucose tolerance, insulin resistance, and increases in IGF-a levels, have cast doubt on hGH’s use as an obesity treatment. However, when it comes to hGH Fragment 176-191, it doesn’t seem to be impacting blood IGF-1 levels or negatively affecting carbohydrate metabolism.

A trial conducted on Zucker rats in 2000 showed no detrimental effects on insulin sensitivity. Also, an investigation on obese mice done in 2001 did not seem to affect insulin secretion.

Properties

Studies conducted on animals suggest that this peptide can exhibit significant theoretical properties, which will be outlined below:

The main potential of this Fragment is its lipolytic properties or, in other words, fat-reducing potential. While growth hormones promote development in infancy, they have also been speculated to have an important purpose in maturity.
Lipoprotein lipase inhibitors may be activated in fat cells,
By stimulating lipolysis in adipocytes may lead to a decrease in fat cell bulk,
It might lead to loss of fat from the host body,

Weight

A 14-day trial researching overweight mice came to a conclusion that Fragment 176-191 may have increased skeletal muscle thermogenesis and boosted fat burning.

The study results indicated that this peptide may have enhanced beta (3)-AR RNA (ADRB3) levels, which caused rapid weight reduction in overweight animals but didn’t have much effect on lean mice.

Cartilage

Based on other animal research, it appears that hGH Fragment 176-191 may boost the effects of hyaluronic acid (HA). When Fragment 176-191 was combined with hyaluronic acid, it might boost cartilage formation in white rabbits which have issues with osteoporosis.

References:

Habibullah MM, Mohan S, Syed NK, Makeen HA, Jamal QMS, Alothaid H, Bantun F, Alhazmi A, Hakamy A, Kaabi YA, Samlan G, Lohani M, Thangavel N, Al-Kasim MA. Human Growth Hormone Fragment 176-191 Peptide Enhances the Toxicity of Doxorubicin-Loaded Chitosan Nanoparticles Against MCF-7 Breast Cancer Cells. Drug Des Devel Ther. 2022 Jun 27;16:1963-1974. doi: 10.2147/DDDT.S367586. PMID: 35783198; PMCID: PMC9249349.

https://www.semanticscholar.org/paper/Human-Growth-Hormone-Fragment-176%E2%80%93191-Peptide-the-Habibullah-Mohan/574cee96c109525005b03688cedaa447ba46b3e8

Habibullah, Mahmoud & Mohan, Syam & Syed, Nabeel & Makeen, Hafiz & Jamal, Qazi & Alothaid, Hani & Bantun, Farkad & Hakamy, Ali & Kaabi, Yahia & Samlan, Ghalia & Lohani, Mohtashim & Thangavel, Neelaveni & Al-Kasim, Mohamed. (2022). Human Growth Hormone Fragment 176–191 Peptide Enhances the Toxicity of Doxorubicin-Loaded Chitosan Nanoparticles Against MCF-7 Breast Cancer Cells. Drug Design, Development and Therapy. 16. 1963. 10.2147/DDDT.S367586.

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Semaglutide (GLP-1) 5mg/10mg $105.00 – $190.00

Semaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist.It is one of the two primary hormones that may enhance incretin activity in rodent models, along with GIP.

GLP-1 is one of the major incretin (gut peptide secreted after nutrient intake) hormones in humans. It plays a pivotal role in many different mechanisms within the body:

Insulin secretion
Inhibits glucagon release (glucagon is secreted as a response in blood sugar drop)
Suppresses hepatic gluconeogenesis (glycogen is the primary carbohydrate stored in the liver)
Delays gastric emptying
Reduces appetite and energy intake

When talking about obese diabetic 2 type patients, GLP-1 assumes a special status in their treatment as it lowers HbA1c levels along with body weight, but without the risk of hypoglycemia.

However, the biggest problem with GLP-1 is its short half-live (of only 1 to 2 minutes) and this is why researchers turner to various other GLP-1 receptor agonists, such as liraglutide, dulaglutide and, of course, semaglutide. Another thing researchers hope to achieve by turning to GLP-1 agonists, such as semaglutide, is to develop an effective diabetes management drug which needs less frequent dosing.

Murine models suggested that semaglutide’s GLP-1 receptor activation affects insulin secretion, blood sugar homeostasis and beta cell protection. Further, in vitro studies showed its potential to also affect glucagon secretion. This insulin glucagon mechanics is what’s used to balance our pancreatic function and regulate metabolism.

References:

Mahapatra MK, Karuppasamy M, Sahoo BM. Semaglutide, a glucagon like peptide-1 receptor agonist with cardiovascular benefits for management of type 2 diabetes. Rev Endocr Metab Disord. 2022 Jun;23(3):521-539. doi: 10.1007/s11154-021-09699-1. Epub 2022 Jan 7. PMID: 34993760; PMCID: PMC8736331.
Meier JJ. GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus. Nat Rev Endocrinol. 2012 Dec;8(12):728-42. doi: 10.1038/nrendo.2012.140. Epub 2012 Sep 4. PMID: 22945360.

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Cagrilintide $145.00 – $255.00

Obesity’s become a global pandemic, currently affecting one third of the entire population, and this is why we can look at it as a chronic disease that requires appropriate treatment.

When talking about obesity, amylin hormone is of great importance as it gets secreted along with insulin and acts as food intake inhibitor, delaying gastric emptying and suppresses post-prandial glucagon responses to meals.

For this reason, there is a tendency to include amylin management in newly developed medication.

And one such compound is cagrilintide – lipidated long-acting amylin analogue.

Though it still hadn’t been thoroughly tested on humans, numerous rat studies showed incredible potential. One such in vitro study involving rats set out to compare cagrilintide’s effectiveness against pramlintide (an FDA-approved diabetes 1/2 medication).

The study showed that pramlintide reduced food intake by 25% in the period of 0-24 hours (it did not cause reduced food intake after 24 hours). But the dosage was substantial – 1000 nmol/kg.

On the other hand, cagrilintide was able to reduce food intake by approximately 50% with a minimal dosage of only 3 nmol/kg. More importantly, this food intake reduction spanned across 60 hours from the moment it was injected.

These results clearly show the potency of cagrilintide in weight loss and diabetes management medication, especially because it acts over such a long time period (allowing subcutaneous injections to be applied once a week).

Reference:

Dehestani B, Stratford NR, le Roux CW. Amylin as a Future Obesity Treatment. J Obes Metab Syndr. 2021 Dec 30;30(4):320-325. doi: 10.7570/jomes21071. PMID: 34929674; PMCID: PMC8735818.

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https://www.sciencedirect.com/topics/medicine-and-dentistry/bremelanotide

PT-141 $55.00

Also called Bremelanotide, PT-141 is a synthetic melanocortin receptor agonist that promotes dopamine release. Since it has such a high affinity for MC4R (Melanocortin 4 Receptor), in the presynaptic neurons of the hypothalamus, it has been approved as a treatment for HSDD (hypoactive sexual desire disorder) in premenopausal women. Under the brand name Vyleesi, Bremelanotide is the first and only FDA-approved way of HSDD treatment.

Sexual Dysfunctions

As we already said, PT-141 is an effective treatment for HSDD in premenopausal women but it’s important to note it should not be used as a treatment in women who already went through menopause or as a way of boosting sexual performance in men. These have not yet been fully tested.

We’ve seen the effectiveness of PT-141 (Bremelanotide) demonstrated in numerous studies. One such study followed female test subjects over the course of 52 weeks where the treated group received a 1.75mg dose right before anticipated sexual intercourse. All participants showed higher scores on general arousal, desire and orgasm, as compared to the placebo group. Also, no major side effects were linked to PT-141 application – the “most severe” ones were nausea, flushing and headache, which only occurred in around 10% of the participants.

Interestingly enough, scientists are still unsure about the Bremelanotide’s exact mechanism of action and how it leads to increased sexual desire in female patients. All we know is that it’s a potent alpha melanocyte-stimulating hormone, binding predominantly to the receptors MC4R and MC1R, and, to a certain extent, to MC1R-MC5R.

PT-141 And Erectile Dysfunction

At the beginning of the article we said that PT-141 (bremelanotide) should not be used to increase sexual desire in men… but this is not entirely true as there is some emerging evidence that this peptide does affect male sexual performance.

Currently, there are a number of effective ED treatment options available. One of the most fail-proof and common ones, incidentally the most invasive one, is an intracavernosal injection – where an injection is applied directly to corpus cavernosum (spongy tissue that runs through the shaft of the penis).

Naturally, researchers are on the lookout for a new, less invasive treatment option and are testing PT-141 as such. Though research is still in its early stages, results showed significant increases in both duration and the erection quality in both “regular” men, as well as those known to be taking viagra.

We still need more research to confirm all these findings and determine the safety and efficacy of using PT-14 as a reliable ED treatment option, but clinical studies suggest we are heading in this direction.

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