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Melanotan-II
Melanotan II was developed at the University of Arizona by a group of researchers led by Victor Hruby and Mac E. Hadley. It is a man made analog of the naturally occurring hormone called melanocortin peptide hormone alpha-melanocyte stimulating hormone, also known as α-MSH. It is supposedly 1000 times more potent than a-MSH. It has been shown to have tanning capability and aphrodisiac effects in the first studies and clinical trials conducted. It is a cyclic lactam analog of α-MSH with the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2. Melanotan-1 was also made to induce certain effects on the body. However, trials show that it does not cause sexual arousal nor have erectile strengthening effects. These aspects are only found in the drugs Melanotan II and bremelanotide aka PT-141.
Till this day the melanotan II peptide has not been approved for use by any governmental drug regulatory bodies such as the FDA for usage outside of clinical trials. Researchers there knew that one of the best defenses against skin cancer was melanin activated via the skin, aka a tan. They hypothesized that an effective way to lower skin cancer rates in people would be to stimulate the body's endogenous pigmentary system to produce a protective layer prior to UV ray exposure. The body's naturally occurring hormone α-MSH causes melanogenesis; it is a process by which the skin's pigment cells produce the skin's pigment also known as melanin. So, researchers decided to test the hypothesis by injecting endogenous a-MSH to the body directly; hoping that it would be a way to sunless tan. They discovered that while the method seems to work, natural α-MSH had a way too short a half life in the body to be practical as a therapeutic form of tanning. Of course they went with a more potent alternative.
Clinical Human Trials
In this study, researchers review their experience with Melanotan II, a non-selective melanocortin receptor agonist, in human subjects with erectile dysfunction (ED). Melanotan II was administered to 20 men with psychogenic and organic ED using a double-blind placebo-controlled crossover design. Penile rigidity was monitored for 6 h using RigiScan. Level of sexual desire and side effects were reported with a questionnaire. In the absence of sexual stimulation, Melanotan II led to penile erection in 17 of 20 men. Subjects experienced a mean of 41 min Rigiscan tip rigidity>80%. Increased sexual desire was reported after 13/19 (68%) doses of Melanotan II vs 4/21 (19%) of placebo (P<0.01). Nausea and yawning were frequently reported side effects due to Melanotan II; at a dose of 0.025 mg/kg, 12.9% of subjects had severe nausea. Researchers conclude that Melanotan II is a potent initiator of penile erection in men with erectile dysfunction. Our findings warrant further investigation of melanocortin agonists and antagonists on penile erection. International Journal of Impotence Research (2000) 12, Suppl 4, S74-S79.
Here is another human study. A pilot phase I study was conducted with a cyclic heptapeptide analog of alpha-melanocyte stimulating hormone (alpha-MSH). The lactam-bridged molecule, called Melanotan-II (MT-II), has the structure Ac-Nle4-Asp5-His6-D-Phe7-Arg8-Trp9-Lys10 alpha-MSH4-10-NH2 (MT-II) and has superpotent melanotropic activity in vitro. A single-blind, alternating day (saline or MT-II), placebo-controlled trial was conducted in 3 normal male volunteers at the starting dose of 0.01 mg/kg of MT-II. Subcutaneous injections of MT-II or saline were given daily (Monday-Friday) for 2 consecutive weeks. Two subjects were escalated by 0.005 mg/kg increments to 0.03 mg/kg and one to 0.025 mg/kg. The 0.03 mg/kg dose produced Grade II somnolence and fatigue in one of two subjects (WHO standards). Mild nausea, not requiring antiemetic treatment, was reported at most MT-II dose levels. A stretching and yawning complex appeared to correlate with the onset of spontaneous, penile erections which were intermittently experienced for 1-5 hours after MT-II dosing, depending on the MT-II dose. Two subjects had increased pigmentation in the face, upper body and buttock, as measured by quantitative reflectance and by visual perception 1 week after MT-II dosing ended. These results demonstrate that MT-II has tanning activity in humans given only 5 low doses every other day by subcutaneous injection. The recommended single MT-II dose for future Phase I studies is 0.025 mg/kg/day.
Melanotan II Helps blood sugar and blood pressure
Previous studies suggest that blockade of melanocortin 3 and 4 receptors (MC3/4-R) markedly attenuates the chronic hypertensive effects of leptin. Although obesity has been reported to be associated with leptin "resistance," it is unclear whether obesity alters the cardiovascular and metabolic effects of chronic MC3/4-R activation. Therefore, we tested whether the cardiovascular and metabolic actions of MC3/4-R activation are attenuated in Sprague-Dawley rats fed a high-fat diet (HF, n=6) compared with rats fed a standard chow (NF, n=6) for 12 months. A 21G steel cannula was placed in the lateral ventricle for ICV infusion, and arterial and venous catheters were implanted for measurement of mean arterial pressure (MAP) 24 hours/day and IV infusions. After a 5-day control period, rats were infused with MC3/4-R agonist melanotan II (10 ng/h, ICV), for 10 days followed by a 5-day recovery period. HF rats were heavier (558+/-21 versus 485+/-13 g) with 140% more visceral fat than NF rats, hyperleptinemic (8.9+/-0.5 versus 2.7+/-0.5 ng/mL), and insulin resistant. HF rats also had higher MAP (109+/-3 versus 100+/-1 mm Hg). Chronic melanotan II infusion significantly increased MAP in HF and NF (7+/-2 and 6+/-1 mm Hg), decreased caloric intake (-32+/-2 and -25 +/-2 kcal/day), and reduced insulin levels in both groups by approximately 50%. Thus, the metabolic and cardiovascular actions of chronic MC3/4-R activation are preserved in diet-induced obesity, supporting a potential role for the hypothalamic melanocortin system in obesity hypertension. (Hypertension. 2006 Feb;47(2):259-64. Epub 2005 Dec 27.) Although this particular effect is not clearly known in humans, further studies done on human are warranted.
Its libido enhancing properties
For most of this article we have gotten into the fact that acts an aphrodisiac. However, we have not exactly explained why. Melanocortins stimulate libido and erection through the forebrain/hindbrain, spinal cord and peripheral area of the brain. Complex interactions between the supraspinal, spinal and peripheral nervous system lead to the highly specific and regulated vasculogenic event of penile erection. Of the many neurotransmitters involved (more so dopamine,gaba, acetylcholine), melanocortins appear to play a significant role in regulation of erection, particularly at the supraspinal and spinal levels. Melanocrotin agents may regulate physiologic erection, and could also have as yet unexplored effects on sexual motivation and libido. Much knowledge has been gained of Melanocortin receptor sites and Melanocortin receptor subtypes involved in erection, particularly through the utilization of new compounds which activate and/or even inhibit specific MC receptors. Melanaton II seems to boost levels of hydrogen sulfate within the brain, the main part of the brain responsible for erection strength/blood retention. However, further detailed studies are necessary, particularly if new therapeutic agents are to be developed. The two super potent synthetic MC agonists, MT-II and PT-141, have been tested in human subjects, with PT-141 showing promise in early clinical trials for treatment of ED. (Peptides. Oct;26(10):1687-9.)
Well it ain’t approved by any governing body that is for sure
Here in 2007, the FDA issued a Warning Letter to an American online vendor illegally marketing melanotan II on the internet as a drug that prevents skin cancer and assists tanning. The FDA has not licensed melanotan II, and explained: "There is no evidence that the product is generally recognized as safe and effective also known as GREASE for its labeled uses." The FDA basically gave a empty warning advising consumers to, "stop using Melanotan II, an unapproved product".
On August 8, 2008 the DMA also issued a warning against the usage of any product called "Melanotan" purchased on the internet, noting that claims that imply that it has an, "effect" for protection against skin cancer, "has not been documented". The DMA further warned that Melanotan has not undergone tests for its effect and possible side effects, and is an "illegal medicinal product" that it is not licensed for usage in the USA or Europe.
The problem is that some of these so called research companies sell peptides are not really claim to be, so the government does not want someone to inject rat poison thinking it’s Melanotan II. I don’t disagree with them on this one as I myself first hand experienced issues with a lack of quality control in which I refuse to allow when I caught it. Counterfeit drugs can either have no effect at all or can be fatal. That is not something that I stand for, now I can assure there are sources that sell reliable Melanotan II. I honestly can say that based on the all research, within due dosage it’s pretty damn safe. You can be the judge; the only thing I see is a slight over stimulation in dopamine and maybe down regulation of your melanin, but again nothing major. Only time will tell, although it does not help that most researchers will not dive too deep into it as with all other peptides. One side effect that I definitely welcome is that surge of sexual urges that comes with this peptide but that is me HEHEHHE.
Melanotan II was developed at the University of Arizona by a group of researchers led by Victor Hruby and Mac E. Hadley. It is a man made analog of the naturally occurring hormone called melanocortin peptide hormone alpha-melanocyte stimulating hormone, also known as α-MSH. It is supposedly 1000 times more potent than a-MSH. It has been shown to have tanning capability and aphrodisiac effects in the first studies and clinical trials conducted. It is a cyclic lactam analog of α-MSH with the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2. Melanotan-1 was also made to induce certain effects on the body. However, trials show that it does not cause sexual arousal nor have erectile strengthening effects. These aspects are only found in the drugs Melanotan II and bremelanotide aka PT-141.
Till this day the melanotan II peptide has not been approved for use by any governmental drug regulatory bodies such as the FDA for usage outside of clinical trials. Researchers there knew that one of the best defenses against skin cancer was melanin activated via the skin, aka a tan. They hypothesized that an effective way to lower skin cancer rates in people would be to stimulate the body's endogenous pigmentary system to produce a protective layer prior to UV ray exposure. The body's naturally occurring hormone α-MSH causes melanogenesis; it is a process by which the skin's pigment cells produce the skin's pigment also known as melanin. So, researchers decided to test the hypothesis by injecting endogenous a-MSH to the body directly; hoping that it would be a way to sunless tan. They discovered that while the method seems to work, natural α-MSH had a way too short a half life in the body to be practical as a therapeutic form of tanning. Of course they went with a more potent alternative.
Clinical Human Trials
In this study, researchers review their experience with Melanotan II, a non-selective melanocortin receptor agonist, in human subjects with erectile dysfunction (ED). Melanotan II was administered to 20 men with psychogenic and organic ED using a double-blind placebo-controlled crossover design. Penile rigidity was monitored for 6 h using RigiScan. Level of sexual desire and side effects were reported with a questionnaire. In the absence of sexual stimulation, Melanotan II led to penile erection in 17 of 20 men. Subjects experienced a mean of 41 min Rigiscan tip rigidity>80%. Increased sexual desire was reported after 13/19 (68%) doses of Melanotan II vs 4/21 (19%) of placebo (P<0.01). Nausea and yawning were frequently reported side effects due to Melanotan II; at a dose of 0.025 mg/kg, 12.9% of subjects had severe nausea. Researchers conclude that Melanotan II is a potent initiator of penile erection in men with erectile dysfunction. Our findings warrant further investigation of melanocortin agonists and antagonists on penile erection. International Journal of Impotence Research (2000) 12, Suppl 4, S74-S79.
Here is another human study. A pilot phase I study was conducted with a cyclic heptapeptide analog of alpha-melanocyte stimulating hormone (alpha-MSH). The lactam-bridged molecule, called Melanotan-II (MT-II), has the structure Ac-Nle4-Asp5-His6-D-Phe7-Arg8-Trp9-Lys10 alpha-MSH4-10-NH2 (MT-II) and has superpotent melanotropic activity in vitro. A single-blind, alternating day (saline or MT-II), placebo-controlled trial was conducted in 3 normal male volunteers at the starting dose of 0.01 mg/kg of MT-II. Subcutaneous injections of MT-II or saline were given daily (Monday-Friday) for 2 consecutive weeks. Two subjects were escalated by 0.005 mg/kg increments to 0.03 mg/kg and one to 0.025 mg/kg. The 0.03 mg/kg dose produced Grade II somnolence and fatigue in one of two subjects (WHO standards). Mild nausea, not requiring antiemetic treatment, was reported at most MT-II dose levels. A stretching and yawning complex appeared to correlate with the onset of spontaneous, penile erections which were intermittently experienced for 1-5 hours after MT-II dosing, depending on the MT-II dose. Two subjects had increased pigmentation in the face, upper body and buttock, as measured by quantitative reflectance and by visual perception 1 week after MT-II dosing ended. These results demonstrate that MT-II has tanning activity in humans given only 5 low doses every other day by subcutaneous injection. The recommended single MT-II dose for future Phase I studies is 0.025 mg/kg/day.
Melanotan II Helps blood sugar and blood pressure
Previous studies suggest that blockade of melanocortin 3 and 4 receptors (MC3/4-R) markedly attenuates the chronic hypertensive effects of leptin. Although obesity has been reported to be associated with leptin "resistance," it is unclear whether obesity alters the cardiovascular and metabolic effects of chronic MC3/4-R activation. Therefore, we tested whether the cardiovascular and metabolic actions of MC3/4-R activation are attenuated in Sprague-Dawley rats fed a high-fat diet (HF, n=6) compared with rats fed a standard chow (NF, n=6) for 12 months. A 21G steel cannula was placed in the lateral ventricle for ICV infusion, and arterial and venous catheters were implanted for measurement of mean arterial pressure (MAP) 24 hours/day and IV infusions. After a 5-day control period, rats were infused with MC3/4-R agonist melanotan II (10 ng/h, ICV), for 10 days followed by a 5-day recovery period. HF rats were heavier (558+/-21 versus 485+/-13 g) with 140% more visceral fat than NF rats, hyperleptinemic (8.9+/-0.5 versus 2.7+/-0.5 ng/mL), and insulin resistant. HF rats also had higher MAP (109+/-3 versus 100+/-1 mm Hg). Chronic melanotan II infusion significantly increased MAP in HF and NF (7+/-2 and 6+/-1 mm Hg), decreased caloric intake (-32+/-2 and -25 +/-2 kcal/day), and reduced insulin levels in both groups by approximately 50%. Thus, the metabolic and cardiovascular actions of chronic MC3/4-R activation are preserved in diet-induced obesity, supporting a potential role for the hypothalamic melanocortin system in obesity hypertension. (Hypertension. 2006 Feb;47(2):259-64. Epub 2005 Dec 27.) Although this particular effect is not clearly known in humans, further studies done on human are warranted.
Its libido enhancing properties
For most of this article we have gotten into the fact that acts an aphrodisiac. However, we have not exactly explained why. Melanocortins stimulate libido and erection through the forebrain/hindbrain, spinal cord and peripheral area of the brain. Complex interactions between the supraspinal, spinal and peripheral nervous system lead to the highly specific and regulated vasculogenic event of penile erection. Of the many neurotransmitters involved (more so dopamine,gaba, acetylcholine), melanocortins appear to play a significant role in regulation of erection, particularly at the supraspinal and spinal levels. Melanocrotin agents may regulate physiologic erection, and could also have as yet unexplored effects on sexual motivation and libido. Much knowledge has been gained of Melanocortin receptor sites and Melanocortin receptor subtypes involved in erection, particularly through the utilization of new compounds which activate and/or even inhibit specific MC receptors. Melanaton II seems to boost levels of hydrogen sulfate within the brain, the main part of the brain responsible for erection strength/blood retention. However, further detailed studies are necessary, particularly if new therapeutic agents are to be developed. The two super potent synthetic MC agonists, MT-II and PT-141, have been tested in human subjects, with PT-141 showing promise in early clinical trials for treatment of ED. (Peptides. Oct;26(10):1687-9.)
Well it ain’t approved by any governing body that is for sure
Here in 2007, the FDA issued a Warning Letter to an American online vendor illegally marketing melanotan II on the internet as a drug that prevents skin cancer and assists tanning. The FDA has not licensed melanotan II, and explained: "There is no evidence that the product is generally recognized as safe and effective also known as GREASE for its labeled uses." The FDA basically gave a empty warning advising consumers to, "stop using Melanotan II, an unapproved product".
On August 8, 2008 the DMA also issued a warning against the usage of any product called "Melanotan" purchased on the internet, noting that claims that imply that it has an, "effect" for protection against skin cancer, "has not been documented". The DMA further warned that Melanotan has not undergone tests for its effect and possible side effects, and is an "illegal medicinal product" that it is not licensed for usage in the USA or Europe.
The problem is that some of these so called research companies sell peptides are not really claim to be, so the government does not want someone to inject rat poison thinking it’s Melanotan II. I don’t disagree with them on this one as I myself first hand experienced issues with a lack of quality control in which I refuse to allow when I caught it. Counterfeit drugs can either have no effect at all or can be fatal. That is not something that I stand for, now I can assure there are sources that sell reliable Melanotan II. I honestly can say that based on the all research, within due dosage it’s pretty damn safe. You can be the judge; the only thing I see is a slight over stimulation in dopamine and maybe down regulation of your melanin, but again nothing major. Only time will tell, although it does not help that most researchers will not dive too deep into it as with all other peptides. One side effect that I definitely welcome is that surge of sexual urges that comes with this peptide but that is me HEHEHHE.
