Institute of Neurobiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
Bioorg Med Chem Lett. 2013 Jul 15;23(14):4052-5. doi: 10.1016/j.bmcl.2013.05.064. Epub 2013 May 28.
We report the synthesis and the biological activity of new analogues of Ac-RFMWMK-NH2 and Ac-RYYRWK-NH2, modified in position 4 and 5, respectively, with incorporation of newly synthesized β(2)-tryptophan analogues. Trp was substituted by the (S)-2-(1-methyl-1H-indol-3-yl)propionic residue or by (S)-2-(5-methoxy-1H-indol-3-yl)propionic residue. The biological activity (pEC50 and Emax) of these compounds was tested on electrically stimulated preparations of rat vas deferens. The 5-methoxy β-tryptophan group reverses the affinity of the compounds.
我们报告了新型 Ac-RFMWMK-NH2 和 Ac-RYYRWK-NH2 类似物的合成和生物活性，这些类似物在 4 位和 5 位进行了修饰，分别引入了新合成的β(2)-色氨酸类似物。色氨酸被 (S)-2-(1-甲基-1H-吲哚-3-基)丙酸残基或 (S)-2-(5-甲氧基-1H-吲哚-3-基)丙酸残基取代。这些化合物的生物活性（pEC50 和 Emax）在大鼠输精管电刺激制剂上进行了测试。5-甲氧基-β-色氨酸基团改变了化合物的亲和力。
