Melanotan-I (MT-I), a ʻoi aku ka pololei [Nle4, D-Phe7]-α-MSH, he analog o α-MSH (melanocyte-stimulating hormone). He laina tridecapeptide, hooikaika ana melanin hoʻokumu ʻana ma o ka hoʻāla koho ʻana o ka MC1R (melanocortin-1 mea loaʻa).
Kākoʻo nā hōʻike hoʻāʻo i kona ʻano mea ʻawaʻawa a me ka ʻole-carcinogenic, i loko o vivo a i loko o nā ʻano like ʻole in vitro. Hoʻohālikelike ʻia me ka α-MSH kūlohelohe, Loaʻa iā Melanotan-I kahi hapalua ola lōʻihi loa; ua kūʻai maikaʻi ʻia ma ka European Union.
Kaʻina
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Helu CAS
75921-69-6
ʻĀpana Molekala
C78H111N21O19
Kaumaha Molecular
1646.85
Noiʻi o Melanotan-I
ʻO ka melanocortin Aia ka ʻōnaehana i ʻelima mau ʻokoʻa ʻokoʻa (MC1-R ma o MC5-R), nā peptides melanocortin i ʻōlelo ʻia (Proopiomelanocortin/POMC nā peptides i loaʻa), a elua nā mea kūʻē kūʻē.
ʻO Melanotan-I hoʻopaʻa koho a hoʻōla i ka mea loaʻa mua, MC1R. ʻO ke kaʻina kumu (Kona-Phe-Arg-Trp) ʻo ia ke kuleana no kēia pilina pili.
ʻO ka hoʻoulu ʻana o ka receptor e alakaʻi i ka intracellular cyclic adenosine monophosphate (kAMP) a me nā mea a pau ma hope PKA-nā ala hilinaʻi; melanin-synthesizing enzymes (ʻO tyrosinase ka laʻana nui) hoʻonui ʻia ka hana.
Hoʻonui eumelanin ʻO ka hana ʻana i loko o ka ʻili e hoʻonui i ka pigmentation – he pale ʻāpana akā waiwai kūʻē i ka ultraviolet a me ke komo ʻana o ke kukui ʻike ʻia. ʻO ka ʻimi ʻana i nā ʻano oxygen reactive i hoʻokomo ʻia e UV (DNA, pūmua, a me ka pōʻino lipid) Ua manaʻoʻiʻo ʻia hoʻi e hoʻopili ʻia e ka eumelanin.
ʻO Melanotan-Ua hoʻohana wau i ka hopena pale nui loa i ka hoʻonui ʻana i kēia eumelanin palekana. Ua ana ʻia kahi hoʻāʻo makapō pālua i nā ʻāpana like ʻole o ka photoprotection; loaʻa nā kumuhana haʻahaʻa i ka sunburn 3 nā pōʻaiapuni o nā ʻinikua subcutaneous.
Ua piʻi ka nui o ka melanin o ka ʻili e like me ka mea i ʻōlelo mua ʻia, a ua hoemiia ka hapa nui o ka epidermal sunburn. Paʻi kiʻi, ma kahi liʻiliʻi loa, he pahuhopu hope koʻikoʻi o ka ʻike ʻana o ka ʻili kanaka i ka UVR.
Melanotan-I induces ili pigmentation in EPP(Erythropoietic Protoporphyria) nā maʻi, e ho'ēmi ana i ka photosensitivity a ma hope iho e hoʻopau i ka ʻeha o ka ʻili.; ka hōʻiliʻili ʻana o kahi photosensitizer, protoporphyrin IX, ke kumu o keia manao i ka malamalama ikeia.
He haʻawina hoʻopaʻa inoa hāmama 4 mālama ʻia nā mahina ma ʻelima mau kumuhana EPP; Ua lawelawe ʻia nā implants Melanotan-I subcutaneous i ka lā 7 a me ka pule 8. Hoʻohālikelike ʻia me ka papa kuhikuhi, ua ana ʻia ka piʻi ʻana o ka melanin ʻili, me ka hoʻomaikaʻi nui ʻana i ka hoʻomanawanui ʻana i ka hoʻoulu māmā – ʻO ka metric kikoʻī i hoʻohana ʻia ʻo ka 'manawa e hiki ai i ka ʻeha hiki ʻole’ malalo o ka malamalama.
ʻO ka ʻAmelika Hui Pū ʻIa. ʻAi a me nā lāʻau lapaʻau (FDA) ʻApono ʻia ʻo Scenesse (afamelanotide), ke ʻano o ka Melanotan-I implant i kēia manawa, no keia mea.
Ua hōʻike nā haʻawina preclinical i ka haʻahaʻa haʻahaʻa (ʻAʻole i ʻike ʻia ka carcinogenicity e like me ka mea i hōʻike ʻia i loko o ka in vitro a me nā mea a pau i hoʻāʻo ʻia ma nā hiʻohiʻona vivo.
ʻO ka hoʻokomo maikaʻi ʻana o ka pigmentation ʻili nui kekahi o nā hopena i kākau maikaʻi ʻia o Melanotan-I; ilihune photoresponsive ʻano ʻili (kokoke i ka pau ʻole ʻana o ka tanning ʻo ia ka hopena) pomaikai nui mai ia mea.
ʻO ka hōʻemi ʻana o ka pane ʻawaʻawa o ka ʻili i ka radiation ultraviolet ka ʻoiaʻiʻo, makemake ʻia ka hopena hope o kēia mau mea a pau – ua hoemi ia ka sunburn a me ka poino pili, ma ka hapa iki, na Melanotan-I.
COA
HPLC
MS
