Witkowska Renata, Chung Nga N, Schiller Peter W, Zabrocki Janusz
Institute of Organic Chemistry, Technical University of Łódź, Łódź, Poland.
J Pept Sci. 2005 Jun;11(6):361-3. doi: 10.1002/psc.620.
To examine the effect on biological activity of replacing D-Cys in the opioid peptide H-Tyr-c[D-Cys-Gly-Phe(pNO(2))-D-Cys]-NH(2) in position 2 or/and 5 with alpha-hydroxymethylcysteine (alpha-Hmc), three analogues were synthesized. These compounds exhibit agonist activity at both mu and delta receptors. However, the most active analogue, with (S)-alpha-Hmc residue in position 5, was 3360- and 2190-fold less active than the parent peptide in the GPI and MVD assays, respectively.
为了研究用α-羟甲基半胱氨酸（α-Hmc）取代阿片肽H-Tyr-c[D-Cys-Gly-Phe(pNO(2))-D-Cys]-NH(2)中第2位和/或第5位的D-半胱氨酸对其生物活性的影响，合成了三种类似物。这些化合物在μ和δ受体上均表现出激动剂活性。然而，在第5位带有（S）-α-Hmc残基的活性最高的类似物，在GPI和MVD试验中的活性分别比母体肽低3360倍和2190倍。
