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EnglishIn order to study the structure-activity relationships of natural opioid deltorphins (H-Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 and H-Tyr-D-Ala-Phe-Asp [or Glu]-Val-Val-Gly-NH2), 15 analogues were synthesized by the solution method. Their activities were determined in binding studies based on displacement of mu- and delta-receptor selective radiolabels from rat brain membranes and in two bioassays, using guinea pig ileum and mouse vas deferens. The obtained data indicate that the high delta-selectivity of deltorphins can be due to the constitution/conformation of the C-terminal part and, at least in part, to preselection by charge.
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| Titolo: | Synthesis and structure-activity relationships of deltorphin analogues |
| Autori: | |
| Data di pubblicazione: | 1991 |
| Rivista: | |
| Citazione: | Synthesis and structure-activity relationships of deltorphin analogues / SALVADORI S; MARASTONI M; BALBONI G; BOREA PA; MORARI M; TOMATIS R. - 34(1991), pp. 1656-1661. |
| Abstract: | In order to study the structure-activity relationships of natural opioid deltorphins (H-Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 and H-Tyr-D-Ala-Phe-Asp [or Glu]-Val-Val-Gly-NH2), 15 analogues were synthesized by the solution method. Their activities were determined in binding studies based on displacement of mu- and delta-receptor selective radiolabels from rat brain membranes and in two bioassays, using guinea pig ileum and mouse vas deferens. The obtained data indicate that the high delta-selectivity of deltorphins can be due to the constitution/conformation of the C-terminal part and, at least in part, to preselection by charge. |
| Handle: | http://hdl.handle.net/11584/6720 |
| Tipologia: | 1.1 Articolo in rivista |
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