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In the present study, two analogues containing N-Me-Gly (Sarcosine, Sar) were synthesized to further investigate the structural-activity relationships of orphanin FQ/nociceptin (OFQ/NC, NC). The replacement of Gly 2 or Gly 3 with Sar increased the flexibility and decreased the hydrophobicity of the N-terminal tetrapeptide. The activity of the analogues was investigated in a series...
This work was designed to observe the effects of nociceptin(13-17), one of the main metabolites of nociceptin (also termed orphanin FQ), in pain modulation at supraspinal level in mice. Intracerebroventricular (i.c.v.) administration of nociceptin/orphanin FQ(13-17) (N/OFQ(13-17)) (5, 0.5, 0.05, 0.005 nmol/mouse) dose-dependently induced potent hyperalgesic effects in the 48 o C warm-water...
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