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.
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2
MOLLICA, ADRIANO;PINNEN, Francesco Enrico;FELICIANI, FEDERICA;CACCIATORE, Ivana;
2010-01-01
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.File in questo prodotto:
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