Njenge-analog yolwakhiwo lwe α-MSH (ihomoni evuselela i-melanocyte), I-Melanotan-II (MT-II) ibonisa iimpawu ezifana ne-α-MSH. Isebenza njengento engakhethiyo melanocortin receptor iagonist, Ukubonisa umsebenzi kwi-melanocortin receptors I-MC1R, MC3R, I-MC4R kwaye MC5R.
Ngokwesakhiwo, I-Melanotan-II ngumjikelo i-heptapeptide (Ac-Nle-cyclo[Asp-His-DPhe-Arg-Trp-Lys]-NH₂). Olu lwakhiwo lwebhayisekile lubonelela ngetsheyini emfutshane yepeptide kune-MT-I engumtya.
Nangona izifundo ze-in vitro zibonisa ukuba iMelanotan-II ibonisa ukusebenza okubuthathaka kuneMelanotan-I ekusebenzeni. i-melanocyte I-MC1R yenza ukuba kubekho umbala, I-Melanotan-II ifunyenwe ineenzuzo ezinokubakho kwezinye izinto, ngakumbi kulawulo lwenkqubo yemithambo-luvo.
Ulandelelwano
AC-{Ngaba}-Asp-Yakhe-{d-Phe}-Arg-Trp-Lys-NH2, (2→7)-lactam
Inombolo yeCAS
121062-08-6
Ifomula yeemolekyuli
I-C50H69N15O9
Ubunzima beMolekyuli
1024.18
Uphando lweMelanotan-II
1.yintoni i-melanotan-II
1)Ukufunyanwa kunye noPhuhliso
I-Melanotan-II i-synthetic melanocortin receptor agonist ekuqaleni yaphuhliswa ukukhusela umhlaza wolusu. Nangona kunjalo, ukufunyaniswa kwayo okungalindelekanga kwenkqubo ye-nervous kunye neziphumo zokulawula umsebenzi wesondo kuye kwandise usetyenziso lwayo olunokwenzeka kwiindawo ezininzi..
2) I-Skin Pigmentation Effects
Njenge-analog ye-α-MSH, I-Melanotan-II inokwenza i-melanocyte isebenze kwaye ibangele ukutshisa ulusu. Kuphononongo olunye olungaboniyo, Abathathi-nxaxheba abathathu bafumana i-saline okanye i-Melanotan-II ngenaliti engaphantsi kwesikhumba kanye yonke imihla phakathi evekini iiveki ezimbini..
Imilinganiselo yaphindwa kwindawo enye ngosuku 21. Uvavanyo olubonakalayo lubonakalise umbala obonakalayo wobuso kubathathi-nxaxheba abalandela ulawulo. Ubungqina bubonisa ukuba i-Melanotan-II ikhuthaza ukutshisa ngesenzo sayo njenge-agonist kwi-MC1R kwi-melanocytes¹.
3)Unyango lwe-Erectile Dysfunction
I-Melanotan-II inokunyanga i-erectile dysfunction yamadoda (ED). Kwiqela elincinci le 10 izigulane ezine-psychogenic ED, inaliti engaphantsi kwesikhumba yepeptide (0.025 mg/kg ubunzima bomzimba) yavavanywa ngokujongwa kwexesha lokwenyani ngaphakathi 6 iiyure: 8 amadoda aphumelele ukwakhiwa okunentsingiselo².
Ezi zinto zifunyanisiweyo ziye zaqinisekiswa kamva kuphononongo olulawulwa ngokuphindiweyo³.
4)Iziphumo zeMetabolic
Izifundo zezilwanyana ziye zabonisa ukuba iMelanotan-II icinezela ukutya kwaye ikhuthaza ukutshiswa kwamafutha. Abaphandi babethe ngokukodwa PTP1B(Iprotheyini iTyrosine Phosphatase 1B) ufuzo (umlawuli ongalunganga wokubonisa i-leptin) kwi I-POMC(Proopiomelanocortin) neurons yeempuku.
Ezimpuku eziguqukayo zibonise iimpendulo ezinamandla iinaliti ze-intracerebroventricular ye leptin kunye neMelanotan-II (i-agonist ye-melanocortin receptor), ukubonakalisa ukuthomalalisa umdla wokutya, ukuhla ukusinda, kwaye Thermogenic iimpendulo.
Ngaphaya koko, oku kucinywa kwemfuzo kukhokelele ekwandisweni kokubonakaliswa kwe-MC4R isamkeli kwiimpuku⁴.
2.Ukuqukumbela
I-Melanotan-II, njenge-agonist engakhethiyo ye-melanocortin receptor, ayibonisi nje kuphela isithembiso sokwenza umbala wolusu kodwa ikwafumene umdla obalulekileyo wesayensi kwiziphumo zayo ezinamandla zokulamla kulawulo lwezesondo., ngakumbi ekuphuculeni i-ED.
Iziphumo zayo zokuqala zeklinikhi kunyango lwe-ED ziyakhuthaza, kwaye yayo ipleiotropic indlela yokusebenza iseka isiseko esithembisayo sophuhliso lwenoveli ye-ED therapeutics.
I-COA
HPLC
NKSK
