Carra' G, Calo' G, Spagnolo B, Guerrini R, Arduin M, Marzola E, Trapella C, Regoli D, Salvadori S
Section of Pharmacology and Neuroscience Centre, Department of Experimental and Clinical Medicine, University of Ferrara, 44100 Ferrara, Italy.
J Pept Res. 2005 Jul;66(1):39-47. doi: 10.1111/j.1399-3011.2005.00272.x.
In the present study we describe the in vitro pharmacological characterization of the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) ligand Ac-RYYRWK-NH2 and the synthesis and biological evaluation of 13 Trp5 substituted Ac-RYYRWK-NH2 analogs. Results indicate that Ac-RYYRWK-NH2 behaves as a highly potent and selective partial agonist at the NOP receptors and that the whole indole moiety of the Trp5 side chain is not required, being a phenyl-ethyl side chain already sufficient for maintaining high potency.
在本研究中，我们描述了痛敏肽/孤啡肽FQ（N/OFQ）受体（NOP）配体Ac-RYYRWK-NH2的体外药理学特性，以及13种色氨酸5取代的Ac-RYYRWK-NH2类似物的合成与生物学评价。结果表明，Ac-RYYRWK-NH2在NOP受体上表现为高效且选择性的部分激动剂，并且色氨酸5侧链的整个吲哚部分并非必需，苯乙基侧链就足以维持高效能。
