A matsayin tsarin analog na α-MSH (melanocyte-stimulating hormone), Melanotan-II (MT-II) yana nuna kaddarorin kama da α-MSH. Yana aiki azaman mara zaɓi melanocortin receptor agonist, yana nuna aiki a masu karɓar melanocortin Saukewa: MC1R, MC3R, Saukewa: MC4R kuma Saukewa: MC5R.
Tsarin tsari, Melanotan-II shi ne cyclic heptapeptide (Ac-Nle-cyclo[Asp-His-DPhe-Arg-Trp-Lys]-NH₂). Wannan gine-ginen da aka yi keke-da-keke yana ba da guntun sarkar peptide fiye da layin MT-I.
Kodayake binciken in vitro ya nuna Melanotan-II yana nuna rashin ƙarfi fiye da Melanotan-I a cikin kunnawa. melanocyte MC1R don haifar da pigmentation, An gano Melanotan-II yana da fa'idodi masu fa'ida a wasu fannoni, musamman a tsarin tsarin juyayi na tsakiya.
Jeri
Ac-{Can}-Asp-Sa-{d-Phe}-Arg-Trp-Lys-NH2, (2→7)-lactam
Lambar CAS
121062-08-6
Tsarin kwayoyin halitta
Saukewa: C50H69N15O9
Nauyin Kwayoyin Halitta
1024.18
Binciken Melanotan-II
1.melanotan-II
1)Ganowa da Ci gaba
Melanotan-II shine melanocortin agonist na roba wanda aka fara haɓaka don kare kansar fata. Duk da haka, Binciken da ba zato ba tsammani na tsarin juyayi na tsakiya da tasirin aikin jima'i ya fadada aikace-aikacen sa a cikin fagage da yawa..
2) Tasirin Pigmentation Skin
A matsayin analog na α-MSH, Melanotan-II na iya kunna melanocytes kuma haifar da fatar fata. A cikin binciken makafi daya, Mahalarta uku sun sami ko dai saline ko Melanotan-II ta hanyar allurar subcutaneous sau ɗaya kowace rana a ranakun mako na makonni biyu.
An maimaita ma'auni a wuri guda a rana 21. Ƙididdigar gani ta bayyana alamun launin fatar fuska a cikin mahalarta bayan gudanarwa. Shaidu sun nuna cewa Melanotan-II yana haɓaka tanning ta hanyar aikinsa a matsayin agonist a MC1R a cikin melanocytes¹.
3)Maganin Ciwon Karuwa
Melanotan-II na iya magance matsalar rashin karfin mazakuta (ED). A cikin ƙaramin ƙungiyar 10 marasa lafiya tare da psychogenic ED, subcutaneous allura na peptide (0.025 mg/kg nauyin jiki) an kimanta ta hanyar saka idanu na ainihi a cikin 6 hours: 8 maza sun samu ma'ana a asibiti².
An tabbatar da waɗannan binciken daga baya a cikin binciken sarrafa makafi biyu³.
4)Tasirin Metabolic
Nazarin dabba sun nuna cewa Melanotan-II yana hana ci kuma yana inganta ƙona mai. Masu bincike na musamman sun fitar da su Saukewa: PTP1B(Protein Tyrosine Phosphatase 1B) kwayoyin halitta (mummunan mai kula da siginar leptin) in Farashin POMC(Proopiomelanocortin) neurons na mice.
Waɗannan berayen mutant sun baje kolin martani mai ƙarfi ga alluran intracerebroventricular na leptin da Melanotan-II (melanocortin agonist mai karɓa), bayyana a matsayin ingantaccen ci abinci, asarar nauyi, kuma thermogenic martani.
Bugu da kari, wannan shafewar kwayoyin halitta ya haifar da ƙara bayyanar mai karɓar MC4R a cikin berayen.
2.Kammalawa
Melanotan-II, a matsayin melanocortin mai karɓar agonist mara zaɓi, Ba wai kawai yana nuna alƙawarin haifar da pigmentation na fata ba amma kuma ya sami babban sha'awar kimiyya don tasirin sa na tsaka-tsaki na tsakiya akan ka'idojin aikin jima'i., musamman a inganta ED.
Sakamakonsa na farko na asibiti a cikin jiyya na ED yana ƙarfafawa, kuma ta pleiotropic Tsarin aiki ya kafa tushe mai ban sha'awa don haɓaka sabbin hanyoyin kwantar da hankali na ED.
COA
HPLC
MS
