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', Giacomo
Primo
;
CALO', Girolamo
Secondo
;
SPAGNOLO, Barbara;GUERRINI, Remo
;
ARDUIN, Marika;MARZOLA, Erika;TRAPELLA, Claudio;REGOLI, Domenico
Penultimo
;
SALVADORI, Severo
Ultimo
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.
2005
Carra', Giacomo; Calo', Girolamo; Spagnolo, Barbara; Guerrini, Remo; Arduin, Marika; Marzola, Erika; Trapella, Claudio; Regoli, Domenico; Salvadori, S...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/470775
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