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.
Tryptophan replacement in the nociceptin/orphanin FQ receptor ligand Ac-RYYRWK-NH2
CARRA', GiacomoPrimo
;CALO', GirolamoSecondo
;SPAGNOLO, Barbara;GUERRINI, Remo
;ARDUIN, Marika;MARZOLA, Erika;TRAPELLA, Claudio;REGOLI, DomenicoPenultimo
;SALVADORI, SeveroUltimo
2005
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.File in questo prodotto:
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