Melanotan-I (MT-I), ma ọ bụ karịa kpọmkwem [Nle4,D-Phe7]-α-MSH, bụ analog nke α-MSH (hormone na-akpali melanocyte). Tridecapeptide linear, ọ na-akwalite melanin guzobe site na-ahọrọ ịgbalite nke MC1R (melanocortin-1 nnabata).
Ihe akaebe nnwale na-akwado profaịlụ ya na-adịghị egbu egbu na nke na-abụghị nke carcinogenic, ma na vivo na ụdị in vitro dị iche iche. Tụnyere α-MSH eke, Melanotan-I nwere ọkara ndụ ogologo oge; a na-ere ya nke ọma na European Union.
Usoro
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Nọmba CAS
75921-69-6
Usoro ihe omimi
C78H111N21O19
Ibu molekụla
1646.85
Nnyocha nke Melanotan-I
Nke melanocortin usoro ihe mejupụtara ise dị iche iche anabata (MC1-R site na MC5-R), peptides nke melanocortin e kwuru n'elu (Proopiomelanocortin/POMC peptides enwetara), na abụọ endogenous antagonists.
Melanotan-M na-ahọrọ nke ọma na-ejikọ ma na-eme ka onye nnata mbụ rụọ ọrụ, MC1R. Isi usoro (His-Phe-Arg-Trp) Ọ bụ ya kpatara mmekọrịta a kapịrị ọnụ.
Nkwalite nnabata na-eduga na intracellular adenosine monophosphate cyclic (cAMP) na ihe niile sochiri PKA-ụzọ dabere; melanin-synthesizing enzymes (tyrosinase bụ isi ihe atụ) na-emecha na-abawanye na ọrụ.
Na-abawanye eumelanin mmepụta n'ime akpụkpọ ahụ na-eme ka pigmenti dịkwuo elu – ihe mgbochi nke nwere akụkụ mana bara uru megide ultraviolet na ntinye ọkụ a na-ahụ anya. Ịchọta ụdị oxygen na-emeghachi omume nke UV (DNA, protein, na mmebi lipid) ekwenyere na eumelanin bụ onye ogbugbo.
Melanotan-I rụpụtara mmetụta nchebe kachasị na ịbawanye eumelanin nchebe a kapịrị ọnụ. Ọnwụnwa kpuru ìsì abụọ tụrụ nha dị iche iche nke fotoprotection; enwetara ihe ndị nwere ike ịnwụ anwụ 3 okirikiri nke subcutaneous injections.
Njupụta melanin akpụkpọ ahụ mụbara dị ka ekwuru na mbụ, na ọtụtụ mkpụrụ ndụ anwụ anwụ epidermal belatara. Nchekwa foto, ọ dịkarịa ala ruo n'ókè dị ịrịba ama, bụ ebumnuche njedebe dị mkpa nke ikpughe akpụkpọ ahụ mmadụ na UVR.
Melanotan-I na-ebute pigmenti anụ ahụ n'ime EPP(Protoporphyria nke erythropoietic) ndị ọrịa, ibelata fotosensitivity na emesịa ibelata mgbu akpụkpọ ahụ metụtara.⁵ EPP n'onwe ya bụ ọrịa mkpụrụ ndụ ihe nketa na-adịghị ahụkebe.; nchịkọta nke fotosensitizer, protoporphyrin IX, na-eme ka uche dị na ìhè a na-ahụ anya.
Ọmụmụ ihe mepere emepe na-agafe 4 E mere ọnwa na isiokwu ise EPP; A na-enye ihe ntinye nke Melanotan-I nke subcutaneous n'ụbọchị 7 na Izu 8. Tụnyere na ntọala, A na-atụle njupụta nke melanin akpụkpọ ahụ, yana nkwado dị ukwuu maka mkpali ọkụ – metric a kapịrị ọnụ ejiri bụrụ 'oge iru mgbu na-enweghị ike ịnagide’ n'okpuru ìhè.
U.S. Nchịkwa nri na ọgwụ (FDA) Scenesse kwadoro (afamelanotide), ụdị ntinye nke Melanotan-I ugbu a, maka nke a kpọmkwem.
Ọmụmụ ihe izizi egosila nsi dị ntakịrị (Ọ dịghị carcinogenicity hụrụ dị ka egosiri na ma in vitro na ihe niile a nwalere na vivo ụdị.
Mmalite nke ọma nke pigmentị akpụkpọ anụ bụ otu n'ime mmetụta nke Melanotan-I nke edekọtara nke ọma; ụdị akpụkpọ ahụ na-adịghị mma na-anabata foto (nso zuru ezu tanning ọdịda bụ ebe njedebe) na-erite uru dị ukwuu na ya.
Mbelata nzaghachi na-egbu egbu nke akpụkpọ ahụ na radieshon ultraviolet bụ eziokwu, N'ihi njedebe nke ihe a niile – ntachu na mmebi ndị metụtara ya na-ebelata, opekata mpe, nke Melanotan-I.
COA
HPLC
MS
