Melanotan II

Melanotan II
Drugi nazivi
  • Ac-Nle-ciklo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2
  • Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH2
  • Ac-ciklo[Nle4, Asp5, D-Phe7, Lys10]α-MSH4–10-NH2
  • N-Acetil-L-norleucil-L-alfa-aspartil-L-histidil- D-Fenilalanil-L-arginil-L-triptofil-L-lizinamid (2->7)-laktam
  • PT-14
Identifikacija
CAS registarski broj 121062-08-6
PubChem[1][2] 92432
MeSH melanotan-II
IUPHAR ligand 1323
Svojstva
Molekulska formula C50H69N15O9
Molarna masa 1024.180

 DaY (šta je ovo?)   (verifikuj)

Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala

Infobox references
3D animacija strukture melanotan II peptidnog molekula

Melanotan II je sintetički analog prirodnog melanokortinskog peptidnog hormona alfa-melanocite stimulišući hormon (α-MSH) za koji je pokazano da ima melanogenezne (potamnjivanje kože) i afrodizijske efekte u preliminarnim studijama i kliničkim ispitivanjima.[3][4][5] On je ciklični laktamski analog α-MSH sa aminokeselinskom sekvencom Ac-Nle-ciklo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2. Melanotanin II je razvijen na univerzitetu Arizone.

Klinička ispitivanja

Pilotna klinička ispitivanja faze I su sprovedena na tri muškarca u Medicinskoj školi, departmana za farmakologiju, univerziteta Arizone u Tusonu, i objavljena 1996. Ustanovljeno je da melanotan II uzrokuje potamnjivanje kože ljudi nakon 5 niskih doza svakog drugog dana putem supkutane injekcije. Nuspojave su blaga mučnina i „istezanje i zevanje“ koji su u korelaciji sa spontanom erekcijama penisa.[6]

Departman za farmakologiju medicinske škole univerziteta Arizone je objavio 1998 studiju u kojoj su učestvovala dva muškarca sa psihogenom impotencijom. Zaključak izveden iz ovog ispitivanja je da je melanotan-II potentan inicijator erekcija kod muškaraca sa psihogenom impotencijom sa podnošljivim nuspojavama u dozama 0.025 mg/kg.[7]

Literatura

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hadley ME (Oct 2005). „Discovery that a melanocortin regulates sexual functions in male and female humans”. Peptides 26 (10): 1687–9. DOI:10.1016/j.peptides.2005.01.023. PMID 15996790. 
  4. ↑ „Tanning drug may find new life as Viagra alternative”. CNN. 1999. Pristupljeno 12. 6. 2008. 
  5. ↑ Jaroff, Leon (20. 6. 1999.). „Tanning Bonus”. Time (magazine). Arhivirano iz originala na datum 2008-07-25. Pristupljeno 17. 9. 2008. 
  6. ↑ Dorr RT, Lines R, Levine N, et al. (1996). „Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study”. Life Sci. 58 (20): 1777–84. DOI:10.1016/0024-3205(96)00160-9. PMID 8637402. 
  7. ↑ Wessells H, Fuciarelli K, Hansen J, et al. (Aug 1998). „Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study”. J Urol. 160 (2): 389–93. DOI:10.1016/S0022-5347(01)62903-3. PMID 9679884. 

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