Enzymatic degradation of carbamoyl-nociceptin analogues

摘要

Nociceptin,a 17-amino acid peptide(FGGFTGARK.SARKLANQ,Noc-(1-17)-OH)is defined as a major product from pro-nociceptin and as the natural endogenous ligand of ORL_1 receptor.N-terminal truncation leads to complete loss of activity.Structure-activity experiments suggest that Noc-(l-13)-OH is the minimum sequence capable of interaction with ORL,receptor.Its amidated analogue possesses the same biological properties as native nociceptin.Like other peptides,nociceptin is degraded by aminopeptidases in plasma to yield primarily Noc-(2-17)-OH and other smaller fragments.