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1 khoom (10Vials)
| Ntim: | |
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▎ Melanotan-2 Structure
Source: PubChem |
Sequence: Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-NH₂ Molecular Formula: C 50H 69N 15O9 Molecular Luj: 1024.2 g / mol CAS Nr .: 121062-08-6 PubChem CID: 92432 Synonyms: MT-II |
▎ Melanotan-2 Kev Tshawb Fawb
Kev tshawb fawb keeb kwm ntawm Melanota yog dab tsi?
Melanota yog ib qho hluavtaws analogue. Nws yog ib qho hluavtaws analogue ntawm α-melanocyte-stimulating hormone (α-MSH), uas yog npaj los ntawm cov tshuaj synthesis txoj kev [1] . α-MSH yog cov tshuaj hormones tshwm sim uas muaj ntau yam kev ua haujlwm ntawm lub cev hauv tib neeg lub cev, suav nrog kev tswj cov tawv nqaij pigmentation. Melanota tau tsim los ua raws li qee qhov kev cuam tshuam ntawm α-MSH tab sis muaj kev ua haujlwm zoo dua thiab cov hom phiaj tshwj xeeb. Melanota tau pib tsim los ua ib yam khoom los txhawb cov tawv nqaij pigmentation, uas yog, hu ua tanning tus neeg sawv cev. Nrog rau kev nce hauv tib neeg qhov kev thov rau tanning, qee cov neeg tau pib nrhiav kom tau cov tawv nqaij sai sai los ntawm kev txhaj tshuaj Melanota . Kev tshawb fawb hauv qhov no feem ntau tsom rau nws cov txheej txheem thiab cuam tshuam rau ntawm daim tawv nqaij pigmentation. Piv txwv li, cov kev tshawb fawb tau pom tias Melanota tuaj yeem khi rau cov receptors tshwj xeeb ntawm melanocytes los txhawb kev tsim cov melanin, yog li ua rau tawv nqaij tsaus [2, 3].
Melanota yog dab tsi?
Melanota yog ib qho hluavtaws analogue uas muaj feem xyuam rau α-melanocyte-stimulating hormone (α-MSH). Nws lub luag haujlwm tseem ceeb yog ua kom cov tawv nqaij pigmentation thiab ua kom tawv nqaij ntawm tib neeg. Melanota feem ntau siv nws cov nyhuv los ntawm kev cuam tshuam nrog melanocortin receptors. Tshwj xeeb, raws li ib qho tsis xaiv melanocortin receptor agonist, nws tuaj yeem txhawb kev tsim cov melanin hauv daim tawv nqaij, yog li ua tiav cov tawv nqaij pigmentation, uas yog, cov nyhuv tanning. Tsis tas li ntawd, nws tseem tuaj yeem tsim cov erection ntawm tus qau thiab cov teebmeem kev sib deev.
Dab tsi yog qhov tshwj xeeb ntawm Melanota hauv tanning?
Melanota induces tawv nqaij tanning los ntawm interacting nrog melanocortin 1 receptor ntawm melanocytes. Nws ntseeg tau tias Melanota ua raws li cov txiaj ntsig ntawm melanocortin α-melanocyte-stimulating hormone (α-MSH) ntawm MC1 receptor ntawm melanocytes, ua rau muaj kev nce hauv kev qhia ntawm agouti signaling protein. Melanota stimulates melanocytes los tsim thiab tso tawm melanin, yog li ua kom tawv nqaij pigmentation [4] . Nws tuaj yeem txhawb kev tsim cov eumelanin hauv daim tawv nqaij kom ua tiav daim tawv nqaij pigmentation. Cov kev tshawb fawb tau pom tias α-melanocyte-stimulating hormone (α-MSH) analogue cyclic -[Ac-Nle(4), Asp(5), D-Phe(7), Lys(10)] alpha-MSH-(4 - 10) amide (Melanota), muaj zog melanocortin receptor agonist [5] ntawm daim tawv nqaij, tuaj yeem txhawb kev tsim cov pigments. .
Dab tsi yog cov txheej txheem tshwj xeeb ntawm Melanota hauv kev ua kom cov penile erection thiab txhawb kev sib deev stimulation?
Induction ntawm erection:
Hauv cov nas tsuag tshuaj loog, Melanota - tsis yog tshwj xeeb melanocortin receptor agonist - nthuav tawm koob tshuaj tiv thaiv erectile induction thaum siv los ntawm kev txhaj tshuaj intravenous (0.1-1 mg / kg) lossis hypothalamic paraventricular nucleus infusion (0.1-1 μg). Cov nyhuv no ua rau cov penile erections thiab txo qhov latency ntawm thawj erectile txheej xwm [6] .Nws cov nyhuv yuav koom nrog activating melanocortin receptors nyob rau hauv lub hauv paus paj hlwb, li no regulating neural pathways ntsig txog erection. Thaum Melanota yog intrathecally txhaj tshuaj (0.2 μg) ntawm qib L6 - S1, lub amplitude ntawm erection txheej xwm yog siab dua. Qhov no qhia tau hais tias txoj hauv kev neural ntawm cov leeg txha caj qaum kuj tseem tuaj yeem koom nrog hauv kev cuam tshuam ntawm erection los ntawm Melanota [6].
Kev txhawb nqa ntawm erection:
Tom qab txhaj tshuaj ntawm Melanota (1 mg / kg), erectile teb raug ntxias los ntawm cavernous paj stimulation yog nce, yog li ua si txhawb lub luag haujlwm hauv erection [6] . Tom qab raug tshem tawm ntawm lub lumbar paravertebral sympathetic saw, txhawb cov nyhuv ntawm Melanota yog abolished. Qhov no qhia tau hais tias qhov kev txhawb nqa ntawm Melanota ntawm erection nyob ntawm kev ncaj ncees ntawm lub lumbar paravertebral sympathetic saw. Hauv qhov sib piv, Melanota txhaj rau hauv corpus cavernosum (1 μg) tsis tau qhia txog kev txhawb nqa. Spinal cord transection los yog ob tog transection ntawm lub plab hlab ntsha los yog cov hlab ntsha dorsal ntawm noov tsis cuam tshuam rau kev txhawb nqa kev ua haujlwm ntawm cov hlab ntsha Melanota (1 mg / kg), qhia ntxiv tias qhov kev txhawb nqa ntawm Melanota ntawm erection yog feem ntau los ntawm txoj kev mob siab rau lub paj hlwb es tsis yog lub pelvic 6..
Txhim kho cov poj niam kev sib deev arousal cwj pwm:
Cov kev tshawb fawb tau pom tias Melanota kuj muaj feem cuam tshuam rau poj niam kev coj cwj pwm. Hauv cov poj niam nas, ovariectomized nas pretreated nrog estradiol benzoate (EB) thiab progesterone (P), intravenous txhaj ntawm Melanota (1 thiab 3 mg / kg) nce tus naj npawb ntawm dhia, rushes, thiab pob ntseg wiggles, qhia tau hais tias progesterone tuaj yeem cuam tshuam nrog Melanota kom nce poj niam tus cwj pwm [7].
Kev cuam tshuam ntawm MTII ntawm cov qog nqaij hlav ntawm melanoma hlwb.
Source: PubMed [1]
Melanota yog ib yam khoom uas muaj ntau yam haujlwm thiab kev tshawb fawb qhia. Cov hauv qab no yuav qhia lwm yam kev tshawb fawb txog Melanota .
Induction ntawm erection:
Hauv qee qhov kev tshawb fawb, nws tau pom tias Melanota kuj muaj feem cuam tshuam rau kev ua me nyuam. Piv txwv li, Melanota tuaj yeem ua rau lub raum tsis zoo. Qee cov neeg mob tau ntsib kev mob erections tom qab txhaj tshuaj subcutaneous ntawm Melanota , thiab tseem pom cov tsos mob ntawm kev mob siab rau lub paj hlwb, xws li lub plawv dhia, nce ntshav siab, tsis xis nyob, thiab tawm hws ntau dhau [8] .Qhov no qhia tau tias Melanota tuaj yeem cuam tshuam rau cov ntshav txaus thiab kev tswj hwm ntawm neural ntawm kev ua me nyuam ntawm cov kab mob hauv nruab nrog cev los ntawm kev hloov pauv ntawm cov receptors tshwj xeeb hauv kev ua haujlwm. erectile muaj nuj nqi. Tsis tas li ntawd, hauv kev tshawb fawb ntawm cov nas tsuag, cov tshuaj melanocortin tuaj yeem ua rau lub cev lordosis, uas yog txhais los ntawm cov pov thawj ntawm kev sib deev arousal [8] , ntxiv hais tias qhov cuam tshuam ntawm Melanota ntawm lub cev xeeb tub yuav cuam tshuam nrog kev sib deev arousal thiab kev tswj ntawm kev sib deev tus cwj pwm.
Kev txhawb nqa ntawm melanin ntau lawm:
Raws li cov khoom siv hluavtaws melanocortin analogue, Melanota tuaj yeem khi rau melanocortin I receptor (MC1R) los txhawb kev tsim melanin [9] .Nws tsuas yog ua tiav qhov no los ntawm kev txhawb nqa kev loj hlob ntawm melanocytes thiab tswj cov haujlwm ntawm tyrosinase. Cov nyhuv no ntawm kev txhawb melanin ntau lawm muab Melanota muaj peev xwm daim ntawv thov tus nqi hauv daim tawv nqaij, piv txwv li, nws tuaj yeem ua lub luag haujlwm hauv kev kho thiab tiv thaiv qee yam kab mob ntawm daim tawv nqaij.
Kev tshawb fawb hauv kev tiv thaiv qog nqaij hlav:
Hauv kev tshawb fawb txog kev tiv thaiv qog, kev tshawb fawb siv B16-F10 melanoma qauv pom tias txawm tias Melanota tsis muaj kev cuam tshuam rau kev loj hlob ntawm melanoma hlwb, nws tuaj yeem cuam tshuam kev tsiv teb tsaws, ntxeem tau, thiab muaj peev xwm tsim muaj peev xwm ntawm melanoma hlwb. Daim ntawv thov hauv zos ntawm Melanota kuj tseem tuaj yeem txo qhov kev mob qog nqaij hlav hauv cov nas nrog tsim melanoma. Nws cov txheej txheem ntawm kev ua haujlwm yog ua kom muaj kev tswj hwm ntawm phosphatase thiab tensin homolog (PTEN) los ntawm melanocortin 1 receptor (MC1R), yog li inhibiting kev loj hlob ntawm melanoma los ntawm downregulating cyclooxygenase II (COX-2) / prostaglandin E2 (PGE2) taw qhia txoj kev [1].
Therapeutic nyhuv ntawm autism:
Qee cov kev tshawb fawb tau siv tus qauv ntawm niam txiv lub cev tiv thaiv kab mob (MIA) nas tus qauv ntawm kev puas siab puas ntsws los ntsuam xyuas cov peev xwm kho mob ntawm melanocortin receptor 4 agonist M Melanota rau cov yam ntxwv zoo li autism hauv cov neeg laus cov nas [10] .Male MIA nas pom cov yam ntxwv zoo li autism, suav nrog kev cuam tshuam kev coj tus cwj pwm, txo kev sib txuas lus, thiab kev sib txuas lus ntau ntxiv. Kev tswj hwm ntawm Melanota rau txiv neej MIA nas rau xya hnub sib law liag ua rau muaj kev txhim kho hauv kev coj tus cwj pwm coj tus cwj pwm. Tsis muaj kev hloov pauv tseem ceeb hauv kev coj tus cwj pwm hauv cov txiv neej C57 nas nrog cov keeb kwm qub tom qab kho nrog Melanota . Tsis tas li ntawd, hauv cov nas C57 ib txwm muaj, tsis muaj kev hloov pauv hauv kev ntxhov siab lossis kev coj cwj pwm rov qab tom qab kev kho mob nrog Melanota, tab sis muaj qhov hnyav ntawm lub cev poob qis tom qab kev kho mob subacute. Cov ntaub ntawv no qhia tau hais tias Melanota yog ib qho tshuaj zoo uas tuaj yeem txhim kho qhov kev coj tus cwj pwm zoo li autism nyob rau hauv tus qauv autism ntawm cov neeg laus txiv neej MIA nas.
Reversal of memory impairment:
Cov kev tshawb fawb tau pom tias kev noj zaub mov muaj roj ntau (HF) tau raug pov thawj los ua kom muaj kev pheej hmoo ntawm cov hlab ntsha puas thiab cov kab mob neurodegenerative. Txoj kev tshawb no tshawb fawb txog kev sib raug zoo ntawm kev noj haus, Melanota tsom rau melanocortin receptors, thiab tus cwj pwm ntawm zebrafish [11] . Kuj ceeb tias, txawm tias lub sijhawm luv luv HF noj zaub mov uas kav ntev li 1% ntawm tus zebrafish lub neej muaj kev cuam tshuam loj heev. Piv nrog zebrafish tau noj cov zaub mov tswj, zebrafish tau noj HF noj zaub mov pom tias tsis muaj kev paub txog kev nco, nce kev ntxhov siab, thiab txo qis kev tshawb nrhiav tom qab tsuas yog peb lub lis piam. Thiab cov kev txawv txav no tshwm sim los ntawm HF noj zaub mov tau thim rov qab los ntawm Melanota . Tsiaj txhu tau noj HF noj thiab kho nrog Melanota pom kev nco, kev ntxhov siab, thiab kev tshawb nrhiav tus cwj pwm zoo ib yam li cov pab pawg tswj. Txoj kev tshawb no muab pov thawj tias txawm tias HF noj zaub mov luv luv tuaj yeem cuam tshuam rau kev nco thiab lub siab, thiab nws yog thawj txoj kev tshawb fawb qhia tias Melanota tuaj yeem thim rov qab cov kev hloov no.
Txoj cai ntawm kev coj tus cwj pwm:
Hauv kev tshawb fawb ntawm neuroscience, nws tau pom tias Melanotan-II tuaj yeem tswj hwm kev coj noj coj ua los ntawm kev txhawb nqa melanocortin receptors thiab tom qab ntawd ua kom lub hauv paus oxytocin [12] . Tshwj xeeb, tom qab kev tswj hwm ntawm Melanota, kev txhaj tshuaj txhaj tshuaj ntau dua li kev tswj hwm intranasal ntawm Melanota tuaj yeem ua rau muaj kev cuam tshuam ntawm Fos hauv cov kab mob magnocellular neurons ntawm supraoptic nucleus (SON) thiab paraventricular nucleus (PVN) ntawm hypothalamus, thiab cov lus teb no tuaj yeem txo qis los ntawm pretreatment nrog 1agonant 1 melanocortin. Electrophysiological cov ntaub ntawv qhia tau hais tias kev txhaj tshuaj ntawm Melanota tuaj yeem ua rau muaj kev sib tw ntawm oxytocin neurons hauv SON. Qhov no qhia tau hais tias Melanota muaj kev tswj hwm ntawm oxytocin system uas cuam tshuam txog kev coj noj coj ua hauv lub paj hlwb, thiab nws cov txheej txheem ntawm kev ua haujlwm yuav yog los tswj cov kev ua ub no thiab tso tawm ntawm oxytocin neurons los ntawm kev ua kom cov receptors tshwj xeeb thiab cov kev taw qhia.
Kev tshawb fawb txog kev rog rog thiab kev noj qab haus huv metabolic:
Hais txog kev rog thiab kev noj qab haus huv hauv metabolic, qee cov kev tshawb fawb tau siv cov qauv caj ces ntawm pituitary adenylate cyclase-activating polypeptide (PACAP)-cov nas uas tsis muaj zog thiab pom tias melanocortin receptor agonist Melanota tuaj yeem ua ib feem cawm tau qhov tsis muaj peev xwm thermogenic ntawm PACAP-tsis muaj nas nas thaum hloov khaub thuas. Qhov no qhia tau hais tias PACAP tuaj yeem ua lub luag haujlwm ntawm cov kab ke melanocortin, tswj cov paj hlwb ua haujlwm ntawm cov nqaij adipose xim av hauv cov nas, yog li muaj kev cuam tshuam rau kev rog rog thiab kev noj qab haus huv [13].
Kev tswj cov metabolism thiab lub cev kub:
Melanota kuj tseem muaj feem cuam tshuam rau cov kab mob endocrine. Piv txwv li, intraperitoneal kev tswj hwm ntawm Melanota rau cov nas tuaj yeem ua rau muaj kev cuam tshuam thiab ntuav hypometabolism/hypothermia [14] .Studies tau pom tias nyob rau hauv nas tsis muaj mast hlwb, lub hypothermia tshwm sim los ntawm Melanota raug tshem tawm, tawm tswv yim tias yuav tsum muaj kev koom tes ntawm mast cells. Melanota ua rau hypothermia nyob rau hauv nas los ntawm activating mast hlwb thiab stimulating histamine 1 receptor, thiab nws cov txheej txheem ntawm kev txiav txim koom nrog kev sib cuam tshuam ntawm ntau yam endocrine yam thiab receptors.
Hauv kev xaus, raws li cov khoom siv hluavtaws uas tau nyiam ntau yam, Melanota nthuav tawm cov yam ntxwv tshwj xeeb hauv ntau qhov chaw. Hauv thaj chaw ntawm daim tawv nqaij, los ntawm kev khi rau cov receptors tshwj xeeb ntawm melanocytes, nws tuaj yeem txhawb kev tsim cov melanin zoo, muab txoj hauv kev uas tsis yog ib txwm ua rau cov neeg uas xav tau lub ntsej muag zoo nkauj. Piv nrog rau tanning los ntawm ntev raug rau ultraviolet rays, Melanota tuaj yeem zam qhov kev puas tsuaj ntawm ultraviolet rays rau ntawm daim tawv nqaij thiab txo cov kev pheej hmoo ntawm tshav kub kub, tawv nqaij laus, thiab txawm tias mob qog noj ntshav.
Los ntawm qhov kev xav ntawm kev tswj hwm kev ua haujlwm ntawm kev sib deev, Melanota muaj txiaj ntsig zoo rau kev ua kom lub cev erection ntawm tus qau thiab pab txhawb kev sib deev. Qhov no yog ib qho kev daws teeb meem zoo rau qee cov neeg uas muaj kev sib deev tsis zoo los yog cov neeg uas vam tias yuav txhim kho lawv txoj kev sib deev. Nws tuaj yeem ua tiav qhov txiaj ntsig zoo ntawm kev ua haujlwm ntawm kev sib deev los ntawm kev ua kom muaj txoj hauv kev neural hauv nruab nrab thiab peripheral paj hlwb thiab tswj hwm cov neurotransmitters thiab receptors, muab cov peev txheej tshiab rau kev txhim kho kev sib deev.
Hauv kev tshawb fawb txog kev rog rog thiab kev noj qab haus huv metabolic, Melanota kuj qhia tau tias muaj txiaj ntsig zoo. Nws tuaj yeem tswj hwm lub zog metabolism thiab lub cev kub thiab muaj qee yam kev txhim kho ntawm kev ua haujlwm tsis zoo ntawm cov ntaub so ntswg adipose hauv kev rog. Nws muab txoj kev tshawb fawb tshiab rau kev kho mob rog rog thiab kev tswj hwm kev noj qab haus huv hauv metabolic, uas yuav pab tau rau kev txhim kho cov tswv yim kho tshiab thiab txhim kho kev noj qab haus huv ntawm cov neeg mob rog rog.
Hais Txog Tus Sau
Cov ntaub ntawv hais saum toj no yog txhua yam tshawb fawb, kho thiab sau los ntawm Cocer Peptides.
Scientific Journal Author
Cousen, P yog tus kws tshawb fawb nrog lub hom phiaj tseem ceeb hauv kev ua xua rau Dermatology Allergy. Nws txoj haujlwm hauv lub tebchaws no tau cuam tshuam nrog ntau lub koom haum, suav nrog South Tees Hosp NHS Fdn Trust, James Cook University Tsev Kho Mob, Royal Cornwall Tsev Kho Mob, University of Sheffield, thiab Chesterfield Royal Hosp. Tshaj nws qhov tshwj xeeb tshwj xeeb hauv Dermatology Allergy, Cousen, P qhov kev tshawb fawb txog kev txaus siab thiab kev ua ub no yuav txuas ntxiv mus rau lwm qhov chaw xws li kev tiv thaiv kab mob, muab qhov kev sib txuas ntawm kev tsis haum tshuaj thiab kev tiv thaiv kab mob. Qhov no yuav suav nrog kev kawm txog cov lus teb tiv thaiv kab mob uas ua rau cov tawv nqaij ua xua thiab tshawb nrhiav cov kev kho tshiab los hloov cov lus teb no.
Tsis tas li ntawd, nws txoj kev tshawb fawb tuaj yeem suav nrog kev sim tshuaj rau cov kev kho mob dermatological tshiab, kev tshawb fawb ntawm daim tawv nqaij barrier muaj nuj nqi thiab nws lub luag haujlwm hauv kev tiv thaiv kev ua xua, thiab kev tshawb nrhiav ntawm cov caj ces uas ua rau tib neeg rau kev ua xua ntawm daim tawv nqaij. Tsis tas li ntawd, xav txog ntau yam kev qhuab qhia ntawm kev tshawb fawb txog kev noj qab haus huv, nws tuaj yeem koom tes nrog cov kws tshaj lij los ntawm lwm qhov chaw xws li pharmacology, microbiology (kawm ntawm daim tawv nqaij microbiome qhov cuam tshuam rau kev ua xua), thiab txawm tias kev puas siab puas ntsws (xws li kev puas siab puas ntsws ntawm cov tawv nqaij ua xua), yog li ua rau muaj kev nkag siab zoo thiab kev tswj hwm ntawm dermatological. Cousen, P tau teev nyob rau hauv qhov kev siv ntawm cov ntaub ntawv pov thawj [4].
