Tryptophan replacement in the nociceptin/orphanin FQ receptor ligand Ac-RYYRWK-NH2.
Tryptophan replacement in the nociceptin/orphanin FQ receptor ligand Ac-RYYRWK-NH2.
复制标题
伤害感受肽/孤啡肽 FQ 受体配体 Ac-RYYRWK-NH2 中的色氨酸替代。
DOI：
10.1111/j.1399-3011.2005.00272.x
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发表时间：
2005
期刊：
影响因子：
--
通讯作者：
Salvadori,S
中科院分区：
文献类型：
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作者：
Carra',G;Calo',G;Spagnolo,B;Guerrini,R;Arduin,M;Marzola,E;Trapella,C;Regoli,D;Salvadori,S
In the present study we describe the in vitro pharmacological characterization of the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) ligand Ac‐RYYRWK‐NH2and the synthesis and biological evaluation of 13 Trp5substituted Ac‐RYYRWK‐NH2analogs. Results indicate that Ac‐RYYRWK‐NH2behaves as a highly potent and selective partial agonist at the NOP receptors and that the whole indole moiety of the Trp5side chain is not required, being a phenyl‐ethyl side chain already sufficient for maintaining high potency.
