Tryptophan replacement in the nociceptin/orphanin FQ receptor ligand Ac-RYYRWK-NH2. |
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| Authors: | G Carra' G Calo' B Spagnolo R Guerrini M Arduin E Marzola C Trapella D Regoli S Salvadori |
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| Affiliation: | Section of Pharmacology and Neuroscience Centre, Department of Experimental and Clinical Medicine, University of Ferrara, 44100 Ferrara, Italy. |
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| Abstract: | 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. |
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