Shevchenko K V, Nagaev I Iu, Alfeeva L Iu, Andreeva L A, Kamenskiĭ A A, Levitskaia N G, Shevchenko V P, Grivennikov I A, Miasoedov N F
Bioorg Khim. 2006 Jan-Feb;32(1):64-70. doi: 10.1134/s1068162006010055.
The radioactive peptide analogue Semax corresponding to the ACTH(4-10) sequence (Met-Glu-His-Phe-Pro-Gly-Pro) with a molar radioactivity of 56 Ci/mmol labeled with tritium at the C-terminal Pro was prepared. The labeled peptide was used for studying the kinetics of Semax penetration into rat brain and blood after its intranasal administration (50 microg/kg, 20 microl of solution) to nonbred white rats of body mass 200-250 g. It was demonstrated that 0.093% of the total introduced radioactivity per gram can be found in the rat brain 2 min after the administration, 80% of this radioactivity belonged to Semax, and the rest, to its metabolites. The peptide undergoes rapid enzymatic degradation, with the tripeptide Pro-Gly-Pro prevailing in biological samples relative to the total content of Semax and its metabolites.
制备了与促肾上腺皮质激素(4-10)序列(Met-Glu-His-Phe-Pro-Gly-Pro)相对应的放射性肽类似物Semax,其摩尔放射性为56 Ci/mmol,在C端脯氨酸处用氚标记。将标记的肽用于研究Semax经鼻给药(50微克/千克,20微升溶液)给体重200-250克的非繁殖白色大鼠后渗透到大鼠脑和血液中的动力学。结果表明,给药后2分钟,每克大鼠脑中可发现引入的总放射性的0.093%,其中80%的放射性属于Semax,其余的属于其代谢产物。该肽经历快速酶促降解,相对于Semax及其代谢产物的总含量,三肽Pro-Gly-Pro在生物样品中占主导地位。