Melanotan-I (MT-I), kapena ndendende [Nle4,D-Phe7]-α-MSH, ndi analogi wa α-MSH (hormone yolimbikitsa melanocyte). Mtundu wa tridecapeptide, zimalimbikitsa melanin mapangidwe kudzera mwa kusankha kutsegula kwa Chithunzi cha MC1R (melanocortin-1 cholandilira).
Umboni woyeserera umatsimikizira mbiri yake yopanda poizoni komanso yopanda carcinogenic, onse mu vivo komanso mumitundu yosiyanasiyana ya vitro. Poyerekeza ndi chilengedwe α-MSH, Melanotan-Ine ndili ndi theka la moyo wautali kwambiri; yagulitsidwa bwino ku European Union.
Kutsatizana
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Nambala ya CAS
75921-69-6
Molecular Formula
C78H111N21O19
Kulemera kwa Maselo
1646.85
Kafukufuku wa Melanotan-I
The melanocortin dongosolo limapangidwa ndi ma receptor asanu osiyanasiyana (MC1-R kudzera Chithunzi cha MC5-R), ma peptides a melanocortin omwe tawatchulawa (Proopiomelanocortin/POMC ma peptides opangidwa), ndi ziwiri antagonists amkati.
Melanotan-I amamangirira ndikuyambitsa cholandilira choyambirira, Chithunzi cha MC1R. Kutsata kwapakati (His-Phe-Arg-Trp) ali ndi udindo pakuchita izi.
Kutsegula kwa receptor kumabweretsa ku intracellular cyclic adenosine monophosphate (CAMP) ndi zonse zotsatila PKA-njira zothandizira; kupanga melanin-synthesizing michere (tyrosinase kukhala chitsanzo chabwino) potsirizira pake amawonjezeka mu ntchito.
Kuwonjezeka eumelanin Kupanga mkati mwa khungu kumapangitsa kuti khungu likhale lolimba – chotchinga pang'ono koma chofunikira polimbana ndi ultraviolet ndi kuwala kowoneka. Kusakaza mitundu ya okosijeni yopangidwa ndi UV (DNA, mapuloteni, ndi kuwonongeka kwa lipid) Amakhulupiriranso kuti amapangidwa ndi eumelanin.
Melanotan-I adateteza kwambiri pakuwonjezera chitetezo cha eumelanin. Kuyesa kwapawiri kwakhungu kuyeza magawo osiyanasiyana achitetezo cha Photoprotection; anthu omwe amakonda kupsa ndi dzuwa amalandila 3 mkombero wa subcutaneous jakisoni.
Khungu la melanin likuwonjezeka monga tanenera kale, ndipo maselo ambiri a epidermal kuwotchedwa ndi dzuwa adachepetsedwa. Kuteteza zithunzi, pamlingo waukulu, ndi cholinga chofunikira chomaliza chakuwonetsa khungu la munthu ku UVR.
Melanotan-I imapangitsa kuti khungu likhale la pigmentation EPP(Erythropoietic Protoporphyria) odwala, kuchepetsa kupenya kwa maso ndi kuchepetsa kupweteka kwapakhungu komwe kumakhudzana.⁵ EPP palokha ndi vuto losowa kwambiri la majini.; kudzikundikira photosensitizer, protophorphyrin IX, zimapangitsa chidwi ichi ku kuwala kowoneka.
Phunziro lotseguka lomwe likupitilira 4 miyezi inachitika pa maphunziro asanu a EPP; subcutaneous Melanotan-I implants inkaperekedwa pa Tsiku 7 ndi Week 8. Poyerekeza ndi zoyambira, Kuwonjezeka kwa kachulukidwe ka melanin pakhungu kunayesedwa, pamodzi ndi kulolerana kwambiri ndi kukondoweza kwa kuwala – metric yomwe imagwiritsidwa ntchito kukhala 'nthawi yofikira zowawa zosapiririka’ pansi pa kuunika.
U.S. Food and Drug Administration (FDA) ovomerezeka Scenesse (afamelanotide), mawonekedwe apano a Melanotan-I implant, kwa cholinga chomwechi.
Maphunziro a preclinical awonetsa kawopsedwe wochepa (palibe carcinogenicity yomwe idawonetsedwa mu vitro komanso zonse zoyesedwa mu vivo.
Kuyika bwino kwa mtundu wowoneka bwino wa khungu ndi chimodzi mwazinthu zodziwika bwino za Melanotan-I.; mtundu wosauka wamtundu wa khungu (pafupi ndi kulephera kofufutira kwathunthu kukhala pomaliza) kupindula kwambiri ndi izo.
Kuchepetsa kuyankha kwapoizoni kwa khungu ku radiation ya ultraviolet ndikowona, zotsatira zofunidwa za zonsezi – kupsa ndi dzuwa ndi kuwonongeka kogwirizanako kumachepetsedwa, osachepera pang'ono, ndi Melanotan-I.
COA
Mtengo wa HPLC
MS
