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1kit (10Vial) .
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▎ Melanotan-2 Struktrɔ
Sos: PubChem |
Sikεns: Ac-Nle-sayklo(Asp-His-D-Phe-Arg-Trp-Lys)-NH2 Mɔlikul Fɔmula: C 50H 69N 15O9 Molikul Weyt: 1024.2 g/mol CAS Nɔmba: 121062-08-6 PubChem CID: 92432. Di wan dɛn we de wok Sinonim dɛn: MT-II |
▎ Melanotan-2 Risach
Wetin na di risach bakgrɔn fɔ Melanota ?
Melanota na wan sintetik analɔg. na sεntetik analכg fכ α-melanocyte-stimulating hormone (α-MSH), we dεn de pripia bay kεmikכl sεntesis mεtכd dεm [1] . α-MSH na כmon we de apin na di nכmal we gεt difrεn fysiolojikal wok dεm na di mכtalman bכdi, inklud fכ rεgεl di skin pigmεntεshכn. Melanota bin disayn fכ miks sכm pan di ifekt dεm we α-MSH de gi bכt i gεt strכng aktiviti εn spεsifi k aplikεshכn pכyzכn. Fɔs, dɛn bin mek mɛlanɔta as sɔntin fɔ mek di skin gɛt kɔlɔ, dat na sɔntin we dɛn kɔl tanning agent. We pipul dɛn bin de aks fɔ tan, sɔm pipul dɛn bigin fɔ tray fɔ gɛt wan tin we go mek dɛn skin dak kwik kwik wan bay we dɛn injekt Mɛlanota . di risach we dεn du pan dis de mεntal fכs pan di mεkanism εn di ifekt we i de du pan di skin pigmεntεshכn. fכ egzampl, stכdi dεm dεn fכnshכn se mεlanota kin tay pan spεsifi k rεsεpכta dεm na di melanosayt dεm fכ mek di melanin prodyuz, we de mek di skin dak [2, 3]..
Wetin na Mɛlanota ?
mεlanota na sεntetik analכg we de riliyt to α-melanosayt-stimulεt כmon (α-MSH). Di men wok we i de du na fɔ mek di skin gɛt mɔ kɔlɔ ɛn fɔ mek mɔtalman skin dak. di mεlanכta de mεntal εksεrt in ifekt bay we i de intarakt wit di melanokכtin rεsεpכta dεm. sכm spεshal wan, as nכn-sεlektiv mεlanokכtin rεsεptכr agonist, i kin mek di prodyushכn fכ melanin na di skin, so dat i kin mek di skin pigmεnt, dat na di tanning ifekt. apat frכm dat, i kin prodyuz spontan penile erection εn sεkswal stimulashכn ifekt dεm bak.
Wetin na di patikyula we aw Mɛlanota de mek pɔsin tan?
melanota de mek di skin tan bay we i de intarakt wit di melanocortin 1 risεptor pan melanosayt dεm. i biliv se Melanota de miks di ifekt we di melanocortin α-melanocyte-stimulating hormone (α-MSH) de gi pan di MC1 risεptor fכ melanocytes, we de rizulta in inkrεs pan di εksprεshכn fכ agouti signal protin. mεlanota de mek di melanosayt dεm fכ prodyuz εn sekret melanin, we de mek di skin kכmכt bכku [4] . i kin mek di yumelanin prodyuz na di skin fכ mek di skin kכmכt. stכdi dεn sho se di α-melanosayt-stimulεt כmon (α-MSH) analכg saykli -[Ac-Nle(4), Asp(5), D-Phe(7), Lys(10)] alfa-MSH-(4 - 10) amid (Melanota ), we na wan pawaful melanocortin rεsεpכta agonist, kin stimulate di prodyushכn fכ yumelanin fכ rich di skin pigmεntεshכn [5] .
wetin na di spεsifi k mεkanism fכ Melanota fכ indyuz penis εrekshכn εn εnhans sεks stimulashכn?
Indukshɔn fɔ erekshɔn:
insay rat dεm we dεn anεsthεt, Melanota —wan nכn spεsifi k melanocortin rεsεptכr agonist — sho di dכz-dipεndεnt εrektil indukshכn we dεn gi am via intravenכs injεkshכn (0.1–1 mg/kg) כ haypothalamic paraventricular nyuklios infushכn (0.1–1 μg). dis ifekt de trigεr di penile erections εn ridyus di latεns fכ fכs erectile ivent dεm [6] .I ifekt kin involv fכ aktibכt melanocortin rεsεpכta dεm na di sεntri nεv sεstem, we de rεgεl di nyural path dεm we riliyt to erection. we dεn injεkt Melanota intratekal (0.2 μg) na di L6 - S1 lεvεl, di amplityuכd fכ di εrekshכn ivent dεm de hכy. dis de sho se di nyural path dεm na di spεnal kכd lεvεl kin involv bak insay di indukshכn fכ erekshכn bay Melanota [6]..
Promoshɔn fɔ erekshɔn:
afta dεn injεkshכn di Melanota (1 mg/kg), di εrektil rεspכns we di kεvεn nεv stimulashכn indyuz de inkrεs, so dat de ple wan prכmot rol fכ εrekshכn [6] . afta dεn akyu rεmov di lכmba paravεrbral simpatik chen, dεn de abolish di prכmot ifekt fכ Melanota. dis sho se di prכmot ifekt we Melanota gεt pan εrekshכn de dipכnt pan di integriti fכ di lכmba paravεrbral simpatik chen. difrεnt frכm dat, Melanota we dεn injεkt insay di kכpas kεvεrnosum (1 μg) nכ sho nכ prכmotεr aktvכti. di spεnal kכd transεkshכn כ baylatarכl transεkshכn fכ di pεlvik nεv כ di dכsal nεv fכ di penis nכ bin impεr di prכmotכn aktiviti fכ intravenכs Melanota (1 mg/kg), we sho fכs se di prכmot ifekt fכ Melanota pan εrekshכn na mεnli tru di simpatik nεv path pas di pεlvik nεv כ di dכsal nεv fכ di penis [6] ..
εnhansmεnt fכ uman sεkswal arousal bihayvya:
Stɔdi dɔn sho se Melanota gɛt impak bak pan uman dɛn we de du mami ɛn dadi biznɛs. pan uman rat dεm, ovariectomized rat dεm we dεn prεtrit wit εstradiol benzoate (EB) εn progesterone (P), intravenous injεkshכn fכ Melanota (1 εn 3 mg/kg) inkrεs di nכmba fכ jכmp, rכsh, εn ia wiggl, we sho se projestεron kin intarakt wit Melanota fכ inkrεs di uman sεks arousal bihayvya [7].
Efεkt כf MTII pan tumorigenicity כf melanoma sεl dεm.
Sos:PubMed [1] we dɛn pul am.
Melanota na wan tin we gɛt bɔku wok ɛn risach dairekshɔn. Di wan dɛn we de kam biɛn ya go introduks ɔda risach dɛn we gɛt fɔ du wit Mɛlanota .
Indukshɔn fɔ erekshɔn:
insay sɔm stכdi dεm, dεn fכnshכn se Melanota gεt impak bak pan di rεprכdaktiv sistεm. fכ egzampl, Melanota kin mek di penis erection abnכmal. Sɔm pasɛnt dɛn bin gɛt pen we dɛn bin de erekshɔn afta dɛn injɛkshɔn Mɛlanota , ɛn dɛn bin sho bak simptom dɛn fɔ simpatik nɛv ɛksayteshɔn, lɛk we dɛn at de bit, we dɛn blɔd prɛshɔn go ɔp, we dɛn nɔ de rɛst, ɛn we dɛn de swet pasmak [8] .Dis sho se Melanota kin afɛkt di blɔd saplai ɛn nyural rɛgyuleshɔn fɔ di riprodaktiv ɔgan dɛn bay we i de akt pan spɛshal nyurotransmitta dεm εn rεsεpכta sistεm dεm, we de mek chenj dεm na di εrektil fכnshכn. pan tap dat, insay stכdi dεm pan rodεnt, melanocortin sכbstans dεm kin mek wan lordosis posture, we dεn intaprit as pruf fכ inkrεs sεkswal arousal [8] , we de sho fכs se di impak we Melanota gεt pan di riprodaktiv sistεm kin riliyt to sεkswal arousal εn di rεguleshכn fכ sεks bihayvya.
Promoshɔn fɔ mek dɛn mek melanin:
as sεntetik mεlanכkכtin analכg, mεlanota kin biεn di melanokכtin I rεsεpכta (MC1R) fכ protεkt melanin prodakshכn [9] .I mεnli achy dis bay we i de promuot di proliferashכn fכ melanosayt dεm εn rεgεl di aktvכti fכ tayrosinase. dis ifekt we de protεkt melanin prodakshכn de gi Melanota pכtεnshal aplikεshכn valyu na di fil fכ di skin, fכ egzampl, i kin ple rol fכ trit εn prεvεnshכn fכ sכm sik dεm na di skin.
Risach pan anti-tumor aspek dɛm:
insay di risach pan anti-tכmכro, stכdi dεm we yuz di B16-F10 melanoma mכdel fכnכt se pan כl we Melanota nכ gεt nכ ifekt pan di proliferashכn fכ di melanoma sεl dεm, i kin ifektivli inhεbit di maygrεshכn, invashכn, εn kכloni fכmeshכn abiliti fכ di melanoma sεl dεm. lokal aplikeshכn fכ Melanota kin כlso sכmtεm attenuate di tכmכro prכgreshכn in mays wit established melanoma. i mεkanism fכ akshכn na fכ mek כprεgulεshכn fכ fכsfataz εn tεnsin homolog (PTEN) tru di melanocortin 1 rεsεpכta (MC1R), we de inhεbit di prכgreshכn fכ melanoma bay we i de dכwnrεgul di sayklooksijenεz II (COX-2)/prostaglandin E2 (PGE2) signal path [1]..
Di tritmɛnt ifɛkt pan ɔtizm:
sכm stכdi dεm yuz wan mεntenal imyun aktibכshכn (MIA) maws mכdel fכ כtizm fכ evaluate di tεrapi pכtεnshal fכ di melanocortin rεsεptכr 4 agonist M Melanota fכ כtizm lεk kכntribyushכn dεm na adכlt man mays dεm [10] .Mal MIA mays dεm sho כtizm-lεk kכntribyushכn dεm, inklud impεriεd soshal bihayvya indikεtכr dεm, rεdכks vכkal kכmyunikeshn, εn inkrεs rεpεtitiv bihayvya. Administreshɔn fɔ Melanota to man MIA mays fɔ sɛvin kɔnsɛkutiv dez bin mek dɛn impruv di sɔshal bihayvya indikɛtɔ dɛn. No signifyant chenj nɔ bin de pan sɔshal bihayvya indikɛtɔ dɛn na man C57 mays dɛn wit nɔmal bakgrɔn afta tritmɛnt wit Melanota . Apat frɔm dat, insay nɔmal C57 mays, nɔ chenj nɔ bin de pan wɔri-layk ɔ ripit bihayvya afta tritmɛnt wit Melanota , bɔt na bin signifyant dɛkɛshɔn pan bɔdi wet afta subakyu tritmɛnt. Dɛn data ya sho se Melanota na wan ifektiv drɔg we kin impruv di ɔtizm-layk bihayvya dɛfisit dɛn na di ɔtizm mɔdel fɔ big man MIA mays dɛn.
Rivεrs כf mεmכri impεryans:
Stɔdi dɔn sho se dɛn dɔn pruv se it we gɛt bɔku fat (HF) kin mek pɔsin gɛt mɔ nerve damej ɛn nyurodijɛnɛraytiv sik dɛn. dis stכdi invεstigat di posεbul rilayshכn bitwin it, Melanota tכgεt melanocortin rεsεpכta dεm, εn di bihayvya fכ zεbra fish [11] . I sɔprayz fɔ no se ivin shɔt tɛm HF it we bin las fɔ lɛk 1% pan di zibra fish in layf bin gɛt strɔng divɛlɔpmɛnt impak. We yu kɔmpia am wit zibra fish we dɛn gi kɔntrol it, zibra fish we dɛn gi HF it sho se dɛn nɔ de mɛmba fayn, dɛn nɔ de wɔri, ɛn dɛn nɔ de du ɛksplɔrɔshɔn afta tri wik nɔmɔ. Ɛn dɛn abnɔmal tin ya we di HF it bin kam wit, Melanota bin rivɛns am . Animal dɛm we dɛn gi HF it ɛn trit wit Melanota sho rɛkɔgnishɔn mɛmori, wɔri, ɛn ɛksplɔrɔshɔn bihayvya we fiba di wan dɛm we di kɔntrol grup bin gɛt. Dis stכdi de gi pruf se ivin fכ sכt tεm HF it kin gεt impak pan mεmכri εn mכd, εn na di fכs stכdi fכ sho se Melanota kin rivεs dεn chenj dεm ya.
Rigyuleshɔn fɔ sɔshal bihayvya:
insay di fild fכ nyurosayns risεch, dεn fכnshכn se Melanotan-II kin rεgεl soshal bihayv bay we i de stimulate melanocortin rεsεpכta dεm εn afta dat i de aktibכt di sεntri כksitosin sistεm [12] . sכm spεshal, afta sistεmik administreshכn fכ Melanota , intravenכs injεkshכn pas intranasal administreshכn fכ Melanota kin sכmtεm indyuz Fos εksprεshכn insay di magnoselular nyuron dεm na di supraoptik nyuklios (SON) εn paraventrikulכr nyuklios (PVN) fכ di haypothalamus, εn dis rεspכns kin atεnuet bay prεtritmεnt wit di melanocortin antagonist SHU-9119 we de na di kɔmni. ilektrofisiolojikal rεkכdin sho se intravenכs injεkshכn fכ Melanota kin inkrεs di fayring rεt fכ כksitosin nyuron dεm na di SON. dis sho se Melanota gεt rεgεdyushכn ifekt pan di כksijεn sistεm we riliyt to soshal bihayvya na di nεv sεstem, εn in mεkanism fכ akshכn kin bi fכ rεgεl di aktvכti εn sekreshכn fכ כksitosin nyuron dεm bay we i de aktibכt spεsifi k rεsεpכta dεm εn signal path dεm.
Risach bɔt fat ɛn mɛtabolik wɛlbɔdi:
in tεm fכ fat εn mεtabolik hεlth, sכm stכdi dεm yuz wan jεnεtik mכdel fכ pituitary adenylate cyclase-activating polypeptide (PACAP)-deficient mays dεm εn dεn fכnshכn se di melanocortin receptor agonist Melanota kin patli rεsכk di impaired thermogenic kapasiti fכ PACAP-deficient mays dεm we dεn de du kol adapteshɔn. dis sho se PACAP kin ple rol apstrim pan di melanocortin sistεm, we de rεgεl di simpatik nεv aktiviti fכ di brawn adipos tisu insay mays, we de mek i gεt impak pan fכ fat εn mεtabolik hεlth [13]..
rεgulεshכn fכ di mεtabolism εn di bכdi tεmprachכ:
Melanota de gεt bכku impak bak pan di εndokrin sistεm. fכ egzampl, intraperitoneal administreshכn fכ Melanota to mays kin mek profaund εn transiεnt haypomεtabolism/haypothermia [14] .Studi dεn sho se insay mays dεm we nכ gεt mast sεl dεm, di haypothεrmia we Melanota kכz de kכmכt, we sho se di patisipeshon fכ mast sεl dεm nid. mεlanota de mek haypothεmia insay mays bay we i de aktibכt di mast sεl dεm εn stimulate di histamin 1 rεsεpכta, εn in mεkanism fכ akshכn involv di intarakshכn bitwin mכltipכl εndokrin fכktכ dεm εn rεsεpכta dεm.
Fɔ dɔn, as sɛntetik sɔbstans we dɔn atrak bɔku atɛnshɔn, Melanota de sho spɛshal kwaliti dɛn pan bɔku fild dɛn. insay di fil fכ di skin, bay we i de biεn spεsifi k rεsεpכta dεm na di melanosayt dεm, i kin ebul fכ protεkt di prodyushכn fכ melanin fayn fayn wan, we de gi wan nכn-tradishכnal tanning mεtכd fכ di wan dεm we want fכ gεt hεlty brכnz kכmpleks. If yu kɔmpia am wit tanning bay we yu de pan ɔltra vayolɛt rayt fɔ lɔng tɛm, Melanota kin avɔyd di dairekt damej we ɔltra vayolɛt rayt de gi yu di skin ɛn i kin ridyus di prɔblɛm dɛn we kin mek yu gɛt san, yu skin ol, ɛn ivin kansa na yu skin.
frכm di pεspεktiv fכ sεkswal fכnshכn rεguleshכn, Melanota gεt bכku ifekt fכ stimulate spontan penile erection εn εnhans sεkswal stimulashכn. Dis na wan fayn sɔlv fɔ sɔm pipul dɛn we nɔ de du mami ɛn dadi biznɛs ɔ di wan dɛn we op fɔ mek dɛn gɛt bɛtɛ ɛkspiriɛns pan mami ɛn dadi biznɛs. i kin ajɔst fayn impak pan sεks fכnshכn bay we i de aktibכt spεsifi k nyural path dεm na di sεntri εn pεrifεral nεv sistεm dεm εn rεgεl di rilayt nyurotransmitta dεm εn rεsεpכta dεm, we de gi nyu posisibilti fכ impruv sεks hεlth.
Insay di risach bɔt fat ɛn mɛtabolik wɛlbɔdi, Melanota sho bak di bɛnifit dɛn we i kin gɛt. i kin ebul fכ rεgεl di εnεji mεtabolism εn di bכdi tεmprachכ εn i gεt sכm improvεmεnt ifekt pan di impεriכs fכnshכn fכ di adipos tisu we fat. I de gi nyu risach dairekshɔn fɔ di tritmɛnt fɔ di wan dɛn we fat ɛn di manejmɛnt fɔ di mɛtabolik wɛlbɔdi, we de ɛp fɔ divɛlɔp nyu tritmɛnt strateji ɛn fɔ mek di wɛlbɔdi stetmɛnt fɔ di wan dɛn we fat bɛtɛ.
Bɔt di pɔsin we rayt di buk
Di tin dɛn we wi dɔn tɔk bɔt ɔp, na ɔl di tin dɛn we Cocer Peptides dɔn du risach, ɛdit ɛn kɔmpilayt.
Sayɛns Jɔnal Author
Cousen, P na risachman wit di praymar fɔs pan di fild fɔ Dɛmatɔlɔji Alɛji. In wok insay dis domɛyn dɔn gɛt fɔ du wit sɔm ɔganayzeshɔn dɛn, lɛk Sawt Tis Hosp NHS Fdn Trɔst, Jems Kuk Yunivasiti Ospital, Royal Kɔnwɔl Ospital, Yunivasiti ɔf Shɛfild, ɛn Chɛstafild Royal Hosp. Biyond in kor spɛshalsayz insay Dɛmatɔlɔji Alɛji, Cousen, P in risach intɛres ɛn aktiviti dɛn go mɔs ɛkstɛnd to rilayt eria dɛn lɛk imyunɔlɔji, we dɛn gi di inhɛrɛnt kɔnekshɔn bitwin alɛji riakshɔn ɛn di imyun sistɛm. dis kin involv fכ stכdi di imyun rεspכns dεm we de lid to alerjik skin kכndishכn dεm εn fכ εksplכr nyu tεrapi we dεn fכ mכdulet dεn rispכns dεm ya.
Apat frɔm dat, in risach kin inklud klinik trial fɔ nyu dɛmatɔlɔjik tritmɛnt dɛm, di stɔdi bɔt di skin barɛri fɔ wok ɛn di wok we i de du fɔ mek dɛn nɔ gɛt alɛji, ɛn di invɛstigeshɔn fɔ di jɛnɛtik tin dɛm we kin mek pɔsin gɛt alɛji na di skin. Dɔn bak, we yu tink bɔt di bɔku bɔku tin dɛn we de apin na di wɛlbɔdi biznɛs, i kin wok wit masta sabi pipul dɛn we kɔmɔt na ɔda say dɛn lɛk famakɔlɔji, maykrobayoloji (we de stɔdi di impak we di skin maykrobayom gɛt pan alɛji), ɛn ivin sayɛns (we de ɛgzamin di saykolojik impak we di alɛji we de mɛn di skin kin gɛt), ɛn dis kin ɛp fɔ mek dɛn ɔndastand ɛn manej di sik dɛn we de mek pɔsin gɛt alɛji fɔ di skin gud gud wan. Cousen, P de list in di rεfrεns כf saytεshכn [4].
