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Melanotan II : ウィキペディア英語版
Melanotan II

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:''Note: this article describes melanotan II which should not be confused with melanotan I which is also known by the standardized name afamelanotide.''
Melanotan II () is a synthetic analogue of the naturally-occurring melanocortin peptide hormone α-melanocyte-stimulating hormone (α-MSH) that in usage has been shown to produce melanogenesis (part of the tanning process that darkens the skin) and have aphrodisiac effects in preliminary studies and clinical trials. Developed at the University of Arizona, it is a cyclic lactam analogue of α-MSH with the amino acid sequence Ac-Nle-''cyclo''()-NH2.
As of 2015, no product containing melanotan II has ever received approval for use from any governmental drug regulatory bodies outside of sanctioned animal and human clinical trials. Unlicensed and untested powders sold as "melanotan II" are found on the Internet and are reported to be used by thousands of members of the general public. Multiple regulatory bodies have warned consumers the peptides may be unsafe and ineffective in usage with one regulatory agency warning that consumers who purchase any product labeled "melanotan" risk buying a counterfeit drug.〔 Medical researchers and Clinuvel Pharmaceuticals, the company developing the related peptide afamelanotide (also known as melanotan I), have warned consumers that counterfeit products sold using the names "melanotan I and II", "pose a hazard to public health".〔(Clinuvel Position Statement ) on counterfeit products. February 10, 2009.〕
==Mechanism of action==
Melanotan II acts as a non-selective agonist of the melanocortin receptors, MC1, MC3, MC4, MC5. Like other melanocortinergic peptides, such as the melanocyte-stimulating hormones (MSHs) and afamelanotide, but unlike adrenocorticotropic hormone (ACTH), melanotan II lacks affinity for the MC2 receptor.〔〔 Reported activity of the drug is as follows:
* MC1 (Ki = 0.686 nM)
* MC2 (Ki > 1000 nM)
* MC3 (Ki = 34.1 nM)
* MC4 (Ki = 6.60 nM
* MC5 (Ki = 46.1 nM)
The melanogenesis produced by melanotan II is caused by activation of the MC1 receptor, whereas its sexual effects are thought to be related to its ability to activate the MC4 receptor (though the MC3 is thought to possibly also be involved).〔〔 Other effects of melanotan II, mostly regarded as adverse effects, include flushing, nausea, vomiting, stretching, yawning, and loss of appetite (the last via activation of MC4).
Melanotan II produces bremelanotide, which, comparatively, is reported to be approximately 50-fold more potent as an inducer of sexual arousal in rats, as an active metabolite.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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