Marastoni M, Salvadori S, Balboni G, Scaranari V, Borea P A, Tomatis A
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Arzneimittelforschung. 1995 Feb;45(2):116-9.
To study the effect of the sulfate ester moiety on the opioid activity, we prepared two tyrosine sulfate-(Tyr(SO3H)-containing dermorphin and deltorphin peptides. 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. In comparison to original peptides and morphine, the obtained data indicate that whereas H-Tyr(SO3H)-D-Ala-Phe-Gly-NH2 shows very minimal interaction with opioid receptors, H-Tyr(SO3H)-D-Ala-Phe-Asp-Val-Val-Gly-NH2 retains a significant activity.
为研究硫酸酯部分对阿片样物质活性的影响，我们制备了两种含硫酸酪氨酸（Tyr(SO3H)）的皮啡肽和德尔托啡肽。基于从大鼠脑膜中置换μ和δ受体选择性放射性标记物的结合研究以及使用豚鼠回肠和小鼠输精管的两种生物测定法，测定了它们的活性。与原始肽和吗啡相比，所得数据表明，虽然H-Tyr(SO3H)-D-Ala-Phe-Gly-NH2与阿片样物质受体的相互作用非常微弱，但H-Tyr(SO3H)-D-Ala-Phe-Asp-Val-Val-Gly-NH2仍保留显著活性。
