Curious about how to take melanotan 2 nasal spray?
Inside, researchers will find what they need to know about administering this sunless tanning and sexual health peptide.
Melanotan-II (MT-II) is a synthetic peptide that mimics the effects of alpha-melanocyte stimulating hormone (α-MSH) to enable sunless tanning.
In addition to its skin-darkening effects, melanotan 2 can increase sexual desire in both men and women, and improve symptoms of erectile dysfunction in men. Fascinatingly, MT-II also modulates metabolism, appetite, and cognition by binding to melanocortin receptors throughout the body.
Although melanotan 2 researchers have primarily favored injections, a nasal spray format may facilitate research if injections are not possible or suboptimal in certain research settings.
In this informative guide, we break down melanotan 2 and include insight on how to administer the peptide via nasal spray. Plus, we include our top recommendation on where to buy research-grade MT-II nasal spray online.
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What is Melanotan 2 Nasal Spray?
Melanotan 2 (MT-II) is a synthetic peptide that non-selectively binds to melanocortin receptors throughout the body, influencing skin pigmentation, sexual arousal, and metabolism .
A melanotan 2 nasal spray is an aqueous suspension of the MT-II peptide that can be delivered intranasally with a metered nasal spray bottle. Importantly, melanotan 2 does not need to be modified to support intranasal delivery and is identical to the peptide used for injection [2, 3] .
The MT-II peptide was originally synthesized and characterized by researchers at the University of Arizona, who sought to develop a synthetic peptide with increased melanogenic activity compared with the endogenous peptide hormone alpha-melanocyte stimulating hormone (α-MSH) .
They made a series of amino acid and chemical modifications to the endogenous 13-amino acid peptide, α-MSH, to generate the highly potent synthetic peptide, melanotan 2 .
Melanotan 2 retains the ability to bind to the melanocortin receptor but with increased affinity and longer duration due to resistance to enzymatic degradation, thus enabling supraphysiological levels of melanogenesis .
Of the five melanocortin receptor subtypes (MC1R-MC5R), melanotan 2 binds to at least MC1R, MCR3, MC4R, and MC5R, similar to α-MSH . Therefore, melanotan 2 is considered a non-selective agonist of melanocortin receptors 1, 3, 4, and 5.
What is Melanotan 2 Nasal Spray Used For?
Melanotan 2 is primarily used for sunless tanning to prevent sun-induced skin damage. In the initial phase I clinical trial for MT-II conducted to evaluate the peptide’s safety and tanning potential, all subjects administered MT-II experienced statistically significant skin darkening . However, the subjects also experienced penile erections shortly after administration, leading study investigators to cease evaluating MT-II for tanning purposes .
Due to the unwanted erection-inducing effects of MT-II, the research team pursued the development of afemelanotide (originally named melanotan 1), which is more expensive to manufacture, but does not induce erections due to an inability to cross the blood-brain barrier. Afemelanotide is now approved by the United States Food and Drug Administration (FDA) to treat the skin disorder erythropoietic protoporphyria .
Notably, melanotan 2 is equally as potent at inducing tanning as afemelanotide, however with added biological effects due to additional binding at melanocortin receptors 3, 4, and 5 [1, 7].
In light of the erection-inducing effects of MT-II, researchers took interest in MT-II’s effects on sexual function and determined that it was a potent treatment for men with psychogenic and organic erectile dysfunction [6, 8].
To make the molecule specific for sexual benefits, researchers made a small chemical modification, changing one -NH2 group to an -OH group [9, 10]. The resulting modified version, called PT-141, is now FDA-approved as a low libido treatment in women .
MT-II is therefore best used when a combination of physiological effects is desired, rather than the specific effects of tanning or sexual arousal alone.
Melanotan 2 Benefits | The A-Z Guide
Since the first clinical trial of melanotan 2 in 1996, researchers have uncovered several benefits of the peptide, many of which were unexpected and related to the newly discovered biology of the melanocortin system [1, 12, 20].
Although many researchers will be familiar with the melanotan 2 benefits on tanning and sexual arousal, the peptide has also been shown to positively impact appetite, insulin sensitivity, and cognition [13, 14, 15, 16].
MT-II and Sunless Tanning
The degree of skin pigmentation, or the level of “tan” is a function of 1) the overall amount of melanin in the skin and 2) the amount of melanin oxidation .
Despite a wide range of skin colors, all humans have almost identical amounts of melanin producing cells called melanocytes. What varies between people of different colors is the amount and specific type of melanin that is produced and transported to neighboring skin cells by melanocytes .
Consequently, light-skinned individuals do not lack the hardware to produce pigment, as they have the same number of melanocytes. They simply have lower levels of activation in their melanocytes and produce more of the yellow-red form of melanin, pheomelanin, which is less UV-protective than eumelanin .
Fortunately for light-skinned individuals who want to get darker without risking damage to their skin, the MT-II peptide binds directly to the melanocortin 1 receptor on melanocytes and stimulates increased production of the darker, more photoprotective eumalanin, thus producing increased pigment and protecting skin without the need for sun exposure [4, 5, 7].
Following an appropriate MT-II dosing protocol, total melanin production will ramp up and be distributed to skin cells leading to a noticeable change in pigment and skin color. However, it is important to note that the shade of the pigment will still change following UV or sun exposure, due to oxidation of eumelanin, which leads to the color associated with the “golden” tan .
In an initial phase I clinical trial, melanotan 2 was shown to increase pigmentation in all subjects included in the study . The peptide has also been shown to be equally as potent at stimulating melanogenesis as the related, FDA-approved peptide called afemelanotide (MT-I) .
Melanotan 2 and Erectile Dysfunction
Benefits of melanotan 2 for erectile dysfunction and sexual activity were unexpectedly discovered during initial clinical evaluations for tanning and skin protection. In the first phase I trial of MT-II, all study participants experienced increased erections following administration of MT-II, causing researchers to refocus MT-II developmental efforts on benefits for sexual activity .
With this new focus, a follow-up study evaluated the effect of melanotan 2 on men with psychogenic erectile dysfunction (ED). Study investigators found that 8 of 10 men suffering from ED reported erections in the six-hour observation period after injection .
Multiple follow-up studies confirmed the ability of MT-II to improve erections in men with erectile dysfunction, including in men with organic ED (caused by physical, rather than psychological problems) [8, 19].
Notably, increased sexual desire was found to be a result of MT-II administration in both studies, a property not found in commonly used phosphodiesterase 5 inhibitors like sildenafil/Viagra .
Researchers subsequently determined that MT-II’s effect on sexual arousal is mediated via interaction with the MC-3 and MC-4 receptors in the central nervous system, which function independently of the MC-1 receptors in melanocytes responsible for tanning .
Melanotan 2 and Demale Sexual Desire
Melanotan 2 can also benefit women with sexual arousal disorders by acting on the MC4R, which has since been established in having a role in regulating sexual function in women [21, 22].
Given the difference in sexual anatomy between males and females, the fact that MT-II is effective in both sexes is related to the fact that it works on melanocortin receptors primarily in the brain, rather than in the periphery [12, 21].
Following licensing of MT-II by Palatin Technologies, the firm developed PT-141, an MT-II derivative that is now FDA-approved under the brand name Vyleesi (bremelanotide) for treatment of low sexual desire in women .
Given the fact that bremelanotide (PT-141) is a naturally-occurring metabolite of MT-II, the extensive literature on PT-141 is relevant in the consideration of MT-II and female sexual desire.
Initial studies of bremelanotide (a metabolite of MT-II) performed with intranasal dosing showed that bremelanotide induced an increase in sexual desire and improvement in satisfaction from sex .
Melanotan 2 and Metabolism
The melanocortin system, and melanotan 2 by extension, also influence metabolism and energy homeostasis [20, 24].
In mice, MT-II was shown to improve peripheral insulin sensitivity independent of diet while also increasing Glut4 mRNA expression in skeletal muscle . In another study conducted in mice, MT-II administration led to a reduction in visceral and subcutaneous fat in mice fed a high-fat diet, primarily through reducing food intake via appetite suppression .
These metabolic effects of MT-II are mediated by binding to MC3R and MC4R, providing another intriguing use case for researchers interested in evaluating the MT-II peptide .
Melanotan 2 and Cognition
Melanotan 2 also appears to have potential benefit on cognition by binding to melanocortin receptors in the brain that are lost over time with age .
The peptide also holds promise in improving sociocognition in disorders like autism spectrum disorder (ASD) by stimulating the release of oxytocin through binding to MC4R. In a mouse model of ASD, administration of MT-II restored social behavior in affected mice .
Melanotan 2 Side Effects
Clinical trials and studies have demonstrated that melanotan 2 is safe and well-tolerated in ED patients and healthy male subjects alike.
Melanotan 2 side effects are generally considered to be minimal and related to dosage [5, 6, 8]. The most common side effects include:
- Facial flushing
- Stomach upset
- Spontaneous erections
Systemic side effects such as flushing, nausea, stomach upset, and fatigue are generally short-lived and tolerable.
Due to the importance of dosage on side effect frequency and intensity, researchers are encouraged to titrate dosing prior to administering MT-II to test subjects and can reference the dosage section below.
Despite the known photoprotective effects of MT-II which are hypothesized to reduce the risks of skin cancer, concerns have paradoxically been raised about a potential cancer risk following publication of an anecdotal case study in which development of melanoma was observed in a patient who used MT-II .
In this case study, the patient also concurrently used tanning beds and authors noted that it was not possible to conclude that MT-II caused the development of melanoma in this patient.
Overall, no causal link has ever been established between MT-II and cancer and importantly, the homologous synthetic peptide, MT-1, is FDA-approved and operates via the same mechanism of action with respect to activation of melanocortin receptors in melanocytes .
Interestingly, there is more recent evidence to support a potential cancer suppressing effect of MT-II independent of photoprotective effects when applied in a topical formulation to melanomas in rodents .
Melanotan 2 Nasal Spray | The A-Z Guide
Since the discovery and initial characterization of melanotan 2 in the late 1980s, subcutaneous injection has been the most common route of administration in part because it was the initial format evaluated in clinical trials [4, 5, 8].
However, the introduction of melanotan 2 nasal sprays offers researchers an additional option for study designs in which injections are unsuitable for reasons including:
- Test subjects uncomfortable with self-administering injections
- Fear of needles
- Injection site pain
- Poor test subject compliance
Although an MT-II nasal spray has not been specifically evaluated in clinical trials, research supports the compatibility of the MT-II peptide with an intranasal format, along with a long track record of delivering peptides and protein intranasally .
There are several FDA-approved nasal sprays that deliver peptides such as oxytocin and desmopressin, and even small proteins like insulin and glucagon [27, 28, 29, 30].
Further, the FDA-approved synthetic peptide bremelanotide, which is a naturally-occurring metabolite of MT-II, has been evaluated in clinical trials in a nasal spray format .
Despite the compatibility of MT-II with a nasal spray format and the advantages of nasal delivery of peptides, there are some important factors to consider to ensure consistent dosing and maximal effectiveness:
- The area within the nasal membrane responsible for absorption is small and can accommodate a relatively limited volume of liquid/aerosol delivered via spray.
- Allow for a sufficient amount of time between sprays in the same nostril to avoid oversaturation and subsequent swallowing of the peptide suspension.
- Use a tilted head position to avoid loss of peptide from the bottom of the nose.
- To maximize absorption, clear nasal congestion as much as possible prior to administering the spray.
- Keep the metered spray pump clean and refrigerated at all times when not in use to minimize degradation of the peptide.
With these guidelines in mind, we will now go over a potential dosing regimen suited for melanotan 2 nasal spray.
Melanotan 2 Nasal Spray Dosage
All dosing of melanotan 2 in clinical trials was performed via subcutaneous injection, with higher and more consistent bioavailability than intranasal spray. As a result, most subjects will require a higher dose of intranasal spray to achieve comparable results to injectable MT-II.
Given the need for titration, experts recommend administering a low initial dose of 0.8mg to evaluate the test subject’s reaction to potential side effects.
Our recommended nasal spray from Amino Asylum delivers 100mcg (i.e. 0.1mg) of MT-II per spray. To achieve the recommended 0.8mg initial dose, this translates to four sprays per nostril, ideally separated by a few minutes between sprays.
After evaluating test subject tolerance, researchers may refer to the following sample melanotan 2 nasal spray dosing protocol for sunless tanning:
- Melanotan 2 Dosage: Administer 1mg of MT-II nasal spray approximately one hour prior to sun or UV exposure. Note that the exact dose will depend on individual sensitivity and preference.
- Frequency: Once every second or third day, depending on individual needs.
- Notes: For lighter skinned subjects, start off with a relatively low amount of sun/UV exposure and slowly build up over time as melanin production ramps up.
By using MT-II in conjunction with UV exposure, test subjects will not only experience a change in skin pigmentation due to increased melanin, but will also achieve the desirable shade of tan that results from UV-induced oxidation of melanin to eumelanin.
Where to Buy Melanotan 2 Nasal Spray Online? | 2023 Guide
Qualified researchers and laboratory professionals may legally purchase melanotan 2 nasal spray online for in vitro testing and laboratory experimentation.
While a number of peptide vendors offer MT-II for sale online, few adhere to rigorous quality control standards while offering their peptides at competitive prices.
Based on our experience, Peptide Sciences offers the best melanotan 2 for injection, while Amino Asylum produces the best melanotan 2 nasal spray on the market.
Assuming you’re looking for a nasal spray product, here is why you should consider Amino Asylum:
- Third-Party Testing: The MT-2 nasal spray and other peptides sold by Amino Asylum are third-party lab tested for quality and purity. This lets customers safely conduct their research without having to worry about contaminated or low-purity products.
- Fair Prices: Amino Asylum offers >99% purity melanotan 2 in a metered spray bottle at $54.99 per 10mg bottle.
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- Customer Care: Amino Asylum staffs professional customer care representatives to handle any customer questions or concerns.
In short, do not hesitate to source your melanotan 2 nasal spray from Amino Asylum.
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Melanotan 2 Nasal Spray | Verdict
Melanotan 2 is a compelling molecule for modulating the melanocortin system and the associated physiology of tanning, sexual arousal, and metabolism.
If maximum consistency in dosing is the top priority, researchers should consider using injectable melanotan 2, as injection offers the best approach for ensuring consistent bioavailability between doses.
But researchers with study designs that are not compatible with injections may prefer the nasal spray format. It is an excellent alternative that offers a validated and well-established route for systemic administration of peptides.
Ultimately, the decision of whether to use injectable MT-II or a nasal spray will come down to the needs of the researcher and the design of the study. That said, a melanotan 2 nasal spray is an excellent option that may be useful in a variety of contexts.
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