Melanotan-I (MT-I), kana zvakanyanya [Nle4,D-Phe7]-α-MSH, iri analogi ye α-MSH (melanocyte-inokurudzira hormone). A linear tridecapeptide, zvinosimudzira melanin kuumbwa kuburikidza nekusarudza activation ye MC1R (melanocortin-1 receptor).
Humbowo hwekuyedza hunotsigira chimiro chayo chisina chepfu uye chisiri checarcinogenic, zvese mu vivo uye mune akasiyana in vitro modhi. Kuenzaniswa neyakasikwa α-MSH, Melanotan-Ini ndine hafu yehupenyu hwakareba; yakabudirira kutengeswa muEuropean Union.
Kutevedzana
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Nhamba yeCAS
75921-69-6
Molecular Formula
C78H111N21O19
Molecular Weight
1646.85
Tsvakurudzo yeMelanotan-I
The melanocortin system inoumbwa neshanu dzakasiyana receptors (MC1-R kuburikidza MC5-R), iyo yambotaurwa melanocortin peptides (Proopiomelanocortin/POMC peptides yakagadzirwa), uye maviri endogenous antagonists.
Melanotan-Ini ndinosarudza inosunga uye inomutsa iyo yekutanga receptor, MC1R. The core sequence (His-Phe-Arg-Trp) ndiyo ine chekuita nekudyidzana uku.
Receptor activation inotungamira kune intracellular Cyclic adenosine monophosphate (camp) uye zvose zvinotevera PKA-nzira dzinoenderana; melanin-synthesizing enzymes (tyrosinase kuva muenzaniso mukuru) pakupedzisira vanowedzerwa mubasa.
Kuwedzera eumelanin kugadzirwa mukati meganda kunoita kuti pigmentation iwedzere – chikamu asi chakakosha chipingamupinyi chinopikisa ultraviolet uye kupenya kwechiedza chinopenya. Kutsvaira kweUV-induced reactive oxygen marudzi (DNA, protein, uye lipid kukuvara) Zvinotendwa zvakare kuti inopindirana ne eumelanin.
Melanotan-I yakaita yakanyanya kudzivirira pakuwedzera iyi inodzivirira eumelanin. Muyedzo wemapofu maviri akayera akasiyana ma paramita e photoprotection; zvidzidzo zvisinganyanyi kupiswa nezuva zvakagamuchirwa 3 kutenderera kwe subcutaneous jekiseni.
Ganda melanin density yakawedzera sezvakambotaurwa, uye masero akawanda epidermal kupisa nezuva akaderedzwa. Photoprotection, pamwero mukuru, chinangwa chakakosha chekupedzisira cheganda remunhu kuratidzwa kuUVR.
Melanotan-I induces ganda pigmentation mukati EPP(Erythropoietic Protoporphyria) varwere, kuderedza photosensitivity uye zvozoderedza marwadzo eganda ane chokuita.⁵ EPP pachayo idambudziko risingawanzowanikwi.; kuunganidzwa kwephotosensitizer, protophorphyrin IX, inokonzera kunzwisiswa uku kune chiedza chinooneka.
Chidzidzo chakavhurika-label chinotenderera 4 mwedzi yakaitwa pazvidzidzo zvishanu zveEPP; subcutaneous Melanotan-I implants yakashandiswa paZuva 7 uye Vhiki 8. Kuenzaniswa nekutanga, kuwedzera kweganda melanin density kwakayerwa, pamwe chete nekuvandudzwa kwakanyanya kushivirira kune kukurudzirwa kwechiedza – iyo chaiyo metric yakashandiswa iri 'nguva yekusvika pakurwadziwa kusingagoneki’ pasi pechiedza.
IU.S. Food and Drug Administration (FDA) Yakabvumirwa Scenesse (afamelanotide), iyo yazvino fomu yeMelanotan-I implant, nokuda kwechikonzero ichochi.
Preclinical zvidzidzo zvakaratidza kuderera kwehuturu (hapana akacherechedza carcinogenicity sezvakaratidzwa mune zvose mu vitro uye zvose zvakaedzwa mu vivo modhi.
Kubudirira induction yeakakosha pigmentation yeganda ndeimwe yeakanyatso kunyorwa mhedzisiro yeMelanotan-I.; murombo photoresponsive ganda marudzi (padhuze nekutadza kusviba kwakakwana kunova magumo) kubatsirwa nazvo zvikuru.
Kudzikiswa kwehupfu hweganda kune ultraviolet mwaranzi ndeyechokwadi, mhedzisiro inodiwa yezvose izvi – kupiswa nezuva uye kukuvara kwakabatana kunoderedzwa, zvimwe zvishoma, naMelanotan-I.
COA
HPLC
MS
