Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2
Articolo
Data di Pubblicazione:
2010
Abstract:
Theopioidagonistsendomorphins(TyreProeTrpePheeNH2;EM1andTyreProePheePheeNH2;EM2)
andmorphiceptin(TyreProePheeProeNH2)exhibitanextremelyhighselectivityfor m-opioidreceptor.
HereaseriesofnovelEM2andmorphiceptinanaloguescontaininginplaceoftheprolineatposition2
the S and R residuesof b-homologuesofproline(HPro),of2-pyrrolidinemethanesulphonicacid(HPrs)
andof3-pyrrolidinesulphonicacid(bPrs)havebeensynthesizedandtheirbindingaffinityandfunctional
activityhavebeeninvestigated.Thehighest m-receptoraffinityisshownby[(S)bPrs
2
]EM2analogue(6e)
whichrepresentsthe firstexampleofa b-sulphonamidoanalogueinthe fieldofopioidpeptides.
andmorphiceptin(TyreProePheeProeNH2)exhibitanextremelyhighselectivityfor m-opioidreceptor.
HereaseriesofnovelEM2andmorphiceptinanaloguescontaininginplaceoftheprolineatposition2
the S and R residuesof b-homologuesofproline(HPro),of2-pyrrolidinemethanesulphonicacid(HPrs)
andof3-pyrrolidinesulphonicacid(bPrs)havebeensynthesizedandtheirbindingaffinityandfunctional
activityhavebeeninvestigated.Thehighest m-receptoraffinityisshownby[(S)bPrs
2
]EM2analogue(6e)
whichrepresentsthe firstexampleofa b-sulphonamidoanalogueinthe fieldofopioidpeptides.
Tipologia CRIS:
1.1 Articolo in rivista
Elenco autori:
Giordano, C; Sansone, A; Masi, A; Lucente, G; Punzi, P; Mollica, Adriano; Pinnen, Francesco Enrico; Feliciani, Federica; Cacciatore, Ivana; Davis, P; Lai, J; Ma, S. W.; Porreca, F; Hruby, V. J.
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