Melanotan-I (MT-I), kapa ka nepo [Nle4,D-Phe7]-α-MSH, ke analoge ea α-MSH (hormone e susumetsang melanocyte). Tridecapeptide e tloaelehileng, e khothalletsa melanin sebopeho ka ho khetha tshebetso ya ho MC1R (melanocortin-1 receptor).
Bopaki ba liteko bo tšehetsa boemo ba eona bo batlang bo se na chefo le bo seng carcinogenic, ka bobeli ka vivo le ka mefuta e fapaneng ea in vitro. Ha ho bapisoa le tlhaho α-MSH, Melanotan-Ke na le halofo ea bophelo bo bolelele haholo; e rekisitsoe ka katleho European Union.
Tatelano
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Nomoro ea CAS
75921-69-6
Foromo ea limolek'hule
C78H111N21O19
Boima ba Molek'hule
1646.85
Lipatlisiso tsa Melanotan-I
The melanocortin tsamaiso e entsoe ka li-receptor tse hlano tse fapaneng (MC1-R ka MC5-R), li-peptide tsa melanocortin tse boletsoeng ka holimo (Proopiomelanocortin/POMC li-peptide tse nkiloeng), le tse peli bahanyetsi ba endogenous.
Melanotan-I ka khetho e tlama le ho kenya tšebetsong mokelikeli oa mantlha, MC1R. Tatelano ya mantlha (His-Phe-Arg-Trp) e ikarabella bakeng sa tšebelisano ena e khethehileng.
Ts'ebetso ea li-receptor e lebisa ho intracellular cyclic adenosine monophosphate (kampo) le tsohle tse latelang PKA-litsela tse itshetlehileng; li-enzyme tse kopanyang melanin (tyrosinase ke mohlala o ka sehloohong) qetellong li eketseha ka ts'ebetso.
Keketseho eumelanin tlhahiso ka har'a letlalo e fella ka ho ntlafatsa mebala – tšitiso e sa fellang empa e le ea bohlokoa khahlanong le ultraviolet le ho kenella ha leseli le bonahalang. Ho tlosoa ha mefuta ea oksijene e hlahisoang ke UV (DNA, protheine, le ho senyeha ha lipid) e boetse e lumeloa hore e kopanngoa ke eumelanin.
Melanotan-I e bile le phello e matla ka ho fetisisa ea tšireletso ho eketsa eumelanin ena e sireletsang. Teko ea bofofu habeli e ile ea lekanya likarolo tse fapaneng tsa ts'ireletso ea foto; ho amohetsoe batho ba tloaetseng ho chesoa ke letsatsi 3 potoloho ea subcutaneous ente.
Letlalo la melanin le eketseha joalo ka ha ho boletsoe pejana, 'me lisele tse ngata tsa epidermal sunburn li fokotsehile. Tšireletso ea lifoto, bonyane ka tekanyo e khōlō, ke sepheo sa bohlokoa sa ho qetela sa ho pepesehela letlalo la motho ho UVR.
Melanotan-I e etsa hore letlalo le be le mebala EPP(Erythropoietic Protoporphyria) bakuli, ho fokotsa ho hlaka ha maikutlo le ho kokobetsa bohloko bo amanang le letlalo.⁵ EPP ka boeona ke lefu le sa tloaelehang la lefutso.; ho bokellana ha photosensitizer, protophorphyrin IX, e bakang kutlo ena kganyeng e bonahalang.
Thuto e bulehileng ea li-label e qala 4 likhoeli li ile tsa etsoa ka lihlooho tse hlano tsa EPP; subcutaneous Melanotan-I implants e ne e tsamaisoa ka Letsatsi 7 le Beke 8. Ha e bapisoa le ea mantlha, ho ile ha lekanyetsoa keketseho ea letsoalo la melanin ea letlalo, mmoho le mamello e ntlafetseng haholo ya ho hlohlelletsa lebone – metric e khethehileng e sebelisoang e le ‘nako ea ho finyella bohloko bo ke keng ba mamelloa’ tlasa kganya.
U.S. Tsamaiso ea Lijo le Lithethefatsi (FDA) Scenesse e amohelehang (afamelanotide), mofuta oa hajoale oa ho kenya Melanotan-I, ka morero ona.
Boithuto ba preclinical bo bonts'itse chefo e batlang e le tlase (ha ho na carcinogenicity e hlokometsoeng joalo ka ha ho bonts'itsoe ho in vitro le tsohle tse lekiloeng ka har'a mefuta ea vivo.
Ho kenella ka katleho ha 'mala oa letlalo oa bohlokoa ke e' ngoe ea litlamorao tse tlalehiloeng hantle tsa Melanotan-I.; mefuta e fokolang ea letlalo e arabelang lifoto (ho hloleha ho fifala ka botlalo ho ba ntlha ya ho qetela) rua molemo haholo ho eona.
Phokotso ea karabelo e chefo ea letlalo mahlaseling a ultraviolet ke 'nete, sephetho se lakatsehang sa tsena tsohle – ho chesoa ke letsatsi le tšenyo e amanang le eona lia fokotseha, bonyane ka mokhoa o itseng, ka Melanotan-I.
COA
HPLC
MOF
