Категории:Меланотан пептиды
Меланотан 2 ИсследованияПередача сигналов меланотан 2 и меланокортин
Меланотан 2 оказывает свое действие путем связывания с рецепторами меланокортина. Существует пять известных рецепторов меланокортина, каждый из которых выполняет разные функции. Известно, что MT-2 связывается в первую очередь с MC-4R и MC-1R, но также слабо связывается с MC-3R.
MC-1R: Обнаруживается на меланоцитах. Стимуляция MC-1R вызывает потемнение кожи и волос.
MC-2R: Обнаруженный в надпочечниках связывание MC-2R способствует секреции гормонов надпочечников, таких как кортизол.
MC-3R: MC-3R участвует в контроле аппетита и регуляции энергии, но об этом рецепторе мало что известно.
MC-4R: Стимуляция MC-4R вызывает изменения в питании и сексуальном поведении. Это также влияет на мужскую эректильную функцию и энергетический гомеостаз.
MC-5R: MC-5R экспрессируется на потовых железах и островковых клетках поджелудочной железы.
Меланотан 2 и аутизм
Новейшие результаты исследования MT-2 показывают, что пептид может обратить вспять некоторые аутистические особенности в широко используемой модели расстройства аутистического спектра (РАС) на мышах. Лечения этого состояния не существует, но недавние исследования показали, что окситоцинтерапия может быть полезна для смягчения некоторых поведенческих проблем, связанных с РАС. Используя мышиную модель материнской иммунной активации, которая, как известно, приводит к аутизму, исследователи исследовали, может ли MT2, который, как известно, стимулирует высвобождение окситоцина, противодействовать РАС или уменьшать распространенное поведение, связанное с РАС. Их исследование показало, что введение MT-2 обращает вспять снижение коммуникации, нарушение социального взаимодействия и повторяющееся поведение, связанное с аутизмом в этой конкретной модели. Фактически, исследователи обнаружили, что введение MT-2 увеличивает экспрессию рецепторов окситоцина в определенных частях мозга, предполагая прямую корреляцию между передачей сигналов окситоцина в этих областях и поведением, специфичным для РАС [1].
These findings not only suggest potential avenues for developing a treatment for ASDthey have helped to define a specific brain pathway that may be integral to thedevelopment of ASD in the first place. These findings could help scientists develop acomplete model of ASD and thus both treatments and preventative measures.
Melanotan 2 and Hunger
There is good evidence to suggest that MT-2 can reduce fat storage and hunger behaviorin animal models. Researchers have found that the melanocortin-4 receptor (MC-4R)plays a role in food preferences and intake and that MT-2 is a potent agonist of MC-4RAdministration of MT-2 to mice causes significant reductions in how much food theyconsume, but also changes their preference for fatty foods. Mice given MT-2 ignore fattyfoods, which they would otherwise prefer. Similarly, mice devoid of the MC-4R receptorconsume fatty foods almost exclusively and are immune to the effects of MT-2[2].
The effects of MT-2 are similar to those of the hormone leptin, sometimes called thesatiety hormone because it reduces cravings and food intake. Leptin, however, has neverbeen useful in the treatment of obesity, even in individuals who are leptin deficient. This islikely because there are two pathways for satiety, called leptin-dependent and leptin-independent pathways. Research suggests MT-2 is more effective in stimulating bothpathways and thus may be a more effective exogenous treatment for reducing hunger[3], [4]. This latter finding has been bolstered by the discovery that thyrotropin-releasinghormone (TRH) gene expression, which has long been known to play a role in the leptin-satiety pathway, is also affected by MC-4R stimulation[5]. Both MT-2 and leptin arethought to cause an increase in TRH expression in the paraventricular nucleus of thehypothalamus, a region of the brain associated with satiety and food intake, but only MT-2 crosses into the centra nervous system in concentrations hiah enouah to have an effecton TRH expression.
Melanotan 2 and Diabetes
The pathogenesis of diabetes is defined by high blood sugar levels, hypersecretion ofglucagon, and the production of ketone bodiesls. it has been known for some time thatleptin counteracts these factors by increasing the uptake of glucose, suppressingglucagon production, and interfering with the pathway that leads to ketone bodyformation. These actions do not depend on insulin and thus leptin signaling is beingactively investigated as an alternative means by which diabetes miaht be treated
Research has revealed that leptin’s effects on blood sugar are regulated throughmelanocortin receptors and that MT-2 produces similar effects[7]. This is significantbecause leptin has its primary effects in the brain but does not cross the blood-brainbarrier as readily as MT-2. Thus, exogenously administered leptin does not reach theCNS in substantial quantities, a fact that reduces its effectiveness as a drug and handsan advantage to MT-2 even though the effects of the two peptides on melanocortinreceptors are nearly identical.
Melanotan 2, lmpulse Control and Alcohol intake
In keeping with the idea that MT-2 may affect oxytocin signaling and thus behavior inASD, research also reveals that the MC-4R receptor may play a role in impulse controlPast studies in rats have shown that administration of MT-2 reduces alcohol intake andincreases water intake even in rats that prefer alcohol[8]. More recently, research hasrevealed that melanotan-2 works synergistically (boosting efficacy more than seven-fold)with naltrexone to blunt binge-like ethanol intake in mice[9].
These findings suggest that MT-2 might not only be an effective treatment in alcoholrelated disorders, but that the peptide is tapping into a more fundamental process ofcraving and desire in the mammalian brain. This research may open up pathways to adeeper understanding not just of alcohol abuse and hunger, but the role of oxytocin inimpulsive behavior. lt may even help researchers identify craving pathways and advanceour understanding of human motivation in aspects of life ranging from work torelationships.
Melanotan 2 and Erectile Dysfunction
Erectile dysfunction (ED) is often attributed to vascular issues and can be effectivelytreated in a majority of men via sildenafil (Viagra) and other drugs that improve blood flowby reducing vascular resistance. Not all ED is due to vascular issues, however, and sosildenafil and similar drugs are ineffective in a small percentage of men and in the vastmajority of women who suffer from hypoactive sexual desire disorder. it has long beenknown that MT-2 is an effective treatment for ED, but research suggests that it may havemore wide-ranging application than drugs like sildenafil due to its actions in the centralnervous system. In a study of men who had failed treatment with Viagra, eighty percentresponded to MT-2 treatment[1o]. MT-2 has been actively investigated in the past as atreatment for both male and female sexual desire disorders.
Melanotan 2 lmpacts Wakefulness
We don’t understand a great deal about sleep and arousal, except that the regulation of consciousness is a complicated part of higher brain function. Research has revealed,however, that several different populations of neurons in the brain are critical to differentaspects of arousal such as sleep onset, depth of consciousness, duration of sleep, andmore. The paraventricular nucleus of the hypothalamus is one area of the brain thatregulates arousal in response to stress, social interaction, feeding, and other cues.
Research using mice shows that stimulation with melanotan 2 increases arousal viainteraction with neuronal fibers of the paraventricular nucleus. in fact, stimulation of thispathway can lead to immediate transition to wakefulness from both NREM and REMsleep[13]. Further research in this area may uncover how to improve sleep and enhanceconcentration via the melanocortin system, making peptides like melanotan 2 potentialnootropics.
Melanotan 2 and Alzheimer’s Disease
Past research has shown that activation of pro-opiomelanocortin (POMC)-derivedneuropeptide can rescue some of the synaptic dysfunction that is caused by theneurofibrillary (amyloid) tangles that arise in Alzheimer’s Disease. POMC-derivedneuropeptide can be activated by melanocortin receptors, so mouse models wereemployed to investigate whether melanotan 2 could be useful in this setting. Thisresearch showed that melanotan 2 substantially reduces amyloid accumulation andprominently reduces the A1 subtype of reactive astrocytes. This latter fact is important because Al astrocytes are thought to be a primary driver of neurotoxicity and neurondeath in Alzheimer’s Disease[14]. These findings suggests that melanocortin activationmay be a potential therapeutic target in Alzheimer’s Disease. This represents a novelpathway for investigating Alzheimer’s Disease treatment and may similarly provide ameans of mitigating neurotoxicity in other degenerative brain diseases.
MT-2 Research
MT-2 is a heavily researched peptide, particularly regarding human behavior, sexualdesire, and impulse control. The peptide, in various forms, has been investigated inclinical trials, though problems with routes of administration have forced scientists back tothe drawing board. There is active and ongoing research into the benefits of this particularpeptide.
MT-2 exhibits minimal to moderate side effects, low oral and excellent subcutaneousbioavailability in mice. Per kg dosage in mice does not scale to humans. MT-2 for sale at PEPTIDE GURUS is limited to educational and scientific research only, not for humanconsumption. Only buy MT-2 if you are a licensed researcher.Автор статьиВышеупомянутая литература была исследована, отредактирована и систематизирована доктором Логаном, доктором медицинских наук. Доктор Логан имеет докторскую степень Медицинской школы Университета Кейс Вестерн Резерв и степень бакалавра в области молекулярной биологии.Научный журналАвторДоктор Уэсселс — профессор Университета Вашингтона, заведующий кафедрой урологии, работал в нескольких национальных и международных профессиональных и правительственных комитетах, включая Международные консультации ВОЗ по эректильной и сексуальной дисфункции, рабочую группу NlDDK по урологическим осложнениям диабета и симпозиум NlH. по диабету. Он хирург, исследователь и эксперт по урогенитальным травмам и эректильной дисфункции. Его клинические интересы включают реконструктивную хирургию мочеполового тракта, лечение острых травм и комплексную хирургию мужской сексуальной дисфункции. Его научные интересы связаны с эпидемиологией и лечением урогенитальных травм; физиология и патофизиология эректильной дисфункции; реконструктивная хирургия; механика травм при авариях и урологические осложнения диабета. Проэректильный агонист меланокортина, разработанный доктором. Уэсселс и его коллеги из Университета Аризоны проводят клинические испытания лечения эректильной дисфункции.
Доктор Уэсселс упоминается как один из ведущих ученых, участвующих в исследованиях и разработках Меланотана 2. Этот врач/ученый никоим образом не одобряет и не пропагандирует покупку, продажу или использование этого продукта по какой-либо причине. Между PEPTIDE GURUS и этим врачом не существует никаких аффилированных или косвенных отношений, подразумеваемых или иных. Цель цитирования доктора — признать, признать и отдать должное исчерпывающим исследованиям и усилиям по разработке, проведенным учеными, изучающими этот пептид. DrWessells указан в [11] и [12] под указанными цитатами.Ссылочные цитаты1.E,Minakova et al..“Melanotan-l reverses autistic features in a maternal immuneactivation mouse model of autism,” PLoS ONE, vol. 14, no. 1, Jan. 2019. [PubMed]
2.A. van der Klaauw et al.. “Role of melanocortin sianaling in the preference fordietary macronutrients in human beings,” Lancet Lond. Engl., vol. 385 Suppl 1, p.S12.Feb.2015.[PubMed]
3.H.Shimizu, K. Inoue, and M. Mori, “The leptin-dependent and -independentmelanocortin signaling system: regulation of feeding and energy expenditure,” J.Endocrinol., vol.193, no.1,pp.1-9,Apr. 2007.[Research Gate]
4.C.Bigrbaek and A.N. Hollenberg,“Leptin and melanocortin siqnaling in thehypothalamus,”Vitam.Horm., vol.65,pp.281-311,2002.[PubMed]
5.F. Guo, K. Bakal, y, Minokoshi, and A.N,Hollenberg,“Leptin Sianaling Targets theThyrotropin-Releasing Hormone Gene Promoter in Vivo,” Endocrinology, vol. 145.no.5,pp.2221-2227,May 2004.[PubMed]
6.Y. H. Lee, M.-Y. Wang, X.-X. Yu, and R. H. Unger, “Glucagon is the key factor inthe development of diabetes,” Diabetologia, vol.59, no.7,pp.1372-1375, 2016[PubMed]
7.C. Toda et al., “Distinct effects of leptin and a melanocortin receptor agonistinjected into medial hypothalamic nuclei on glucose uptake in peripheral tissues,Diabetes, vol.58,no.12,pp.2757-2765,Dec.2009.[PubMed]
8.D.A. York, S. Boghossian, and M. Park-York, “Melanocortin activity in theamygdala influences alcohol intake,” Pharmacol. Biochem. Behav.. vol. 98. no, 1pp.112-119,Mar.2011.[PubMed]
9.M. Navarro, F. Carvajal, J.M. Lerma-Cabrera, l. Cubero, M. J. Picker, and T. E.Thiele, “Evidence that Melanocortin Receptor Agonist Melanotan-ll SynergisticallyAugments the Ability of Naltrexone to Blunt Binge-Like Ethanol Intake in MaleC57BL/6J Mice,”Alcohol. Clin.Exp.Res., vol. 39, no.8, pp.1425-1433,Aug.2015.[PubMed]
10.”Synthetic melanotropic peptide initiates erections in men with psychogenic erectiledysfunction: double-blind, placebo controlled crossover study. – PubMed – NCBl.”[Onlinel.Available: https://www.ncbi.nlm.nih.gov/pubmed/9679884.[Accessed: 15May-2019].
11.WESSELLS, H. , HRUBY, V. J., HACKETT, J., HAN,G., BALSE-SRINIVASAN, Pand VANDERAH, T. W. (2003), MT-l Induces Penile Erection via Brain and SpinalMechanisms. Annals of the New York Academy of Sciences, 994: 90-95.doi:10.1111/i.1749-6632.2003.tb03166.x
12.Wessells, H.(1998).Synthetic melanotropic peptide initiates erections in men withpsychogenic erectile dysfunction: Doubleblind placebo controlled crossover studyNature.com.Available at: https://www.nature.com/articles/3900371.pdf
13.M.T. lslam et a., “Vasopressin neurons in the paraventricular hypothalamuspromote wakefulness via lateral hypothalamic orexin neurons,” Curr. Biol. CB, ppS0960-9822(22)01121-6,Jul.2022,doi: 10.1016/i.cub.2022.07.020.[PubMed]
14.J.K. Y. Lau et a/., “Melanocortin receptor activation alleviates amyloid pathologyand glial reactivity in an Alzheimer’s disease transgenic mouse model,” Sci. Rep.vol.11,no.1,p.4359,Feb.2021, doi: 10.1038/s41598-021-83932-4.[PubMed]
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The products offered on this website are furnished for in-vitro studies only. In-vitro studies(Latin: in glass) are performed outside of the body. These products are not medicines ordrugs and have not been approved by the FDA to prevent, treat or cure any medicalcondition, ailment or disease, Bodily introduction of any kind into humans or animals isstrictly forbidden by law.
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