生物活性

• 描述Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Nociceptin (1 μg/mL) significantly prevents LPS (10 ng/mL)-stimulated cell migration whereas it is ineffective when added alone. Nociceptin (1 nM-10 μM) elicits a concentration-dependent blockade of LPS-mediated cell migration, with a maximal effect at 1 and 10 μM. Nociceptin counteracts LPS-induced elevation of IL-1β mRNA levels. Nociceptin (1 μM) and NNC 55-0396 induce apoptotic cell death in U87 cells. Nociceptin (1 μM) counteracts LPS-induced [Ca2+]i increase in U87 cells via β-arrestin 2. Nociceptin counteracts the LPS-induced phosphorylation of PKC and ERK in U87 cells. Nociceptin inhibits the LPS-mediated transcriptional activation of NF-kB and AP-1 reporter genes^[1]. The i.v. administration of nociceptin (10-100 nmol/kg) inhibits the micturition reflex in a naloxone-resistant manner. Intrathecal nociceptin (10 nmol/rat) produces urodynamic modifications similar to those induced by the i.v. administration. Intracerebroventricular (i.c.v.) administration of nociceptin (0.3-1 nmol/rat) also inhibited the micturition reflex in a naloxone-resistant manner suggesting a direct effect on supraspinal sites controlling the micturition. The application of nociceptin (5-50 nmol/rat) onto the bladder serosa when the intravesical volume was subthreshold for the triggering of the micturition reflex, activated the reflex in a dose-dependent manner; the same treatment produced a biphasic effect on the ongoing reflex^[2]. Injection of nociceptin into mice stimulated Rec8 phosphorylation and meiotic chromosome dynamics in testes, whereas injection of nocistatin, a specific inhibitor for nociceptin, abolished them^[3].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03193398	Major Depressive Disorder	Phase 2	Active, not recruiting	December 2018	United States, California ... more >> United States Cerritos, California, United States, 90703 United States Garden Grove, California, United States, 92845 United States, Florida United States, Florida Jacksonville, Florida, United States, 32256 United States Lauderhill, Florida, United States, 33319 United States, Florida Orlando, Florida, United States, 32801 United States, Illinois United States Libertyville, Illinois, United States, 60048 United States, New York United States Rochester, New York, United States, 14618 United States, Tennessee United States Memphis, Tennessee, United States, 38119 Collapse <<
  NCT03302416	Healthy	Early Phase 1	Recruiting	June 1, 2019	United States, Pennsylvania ... more >> University of Pittsburgh Recruiting Pittsburgh, Pennsylvania, United States, 15213 Collapse <<
  NCT00173225	-	-	Unknown	-	Taiwan ... more >> Ping-Hung Kuo Recruiting Taipei, Taiwan, 100 Contact: Ping-Hung Kuo, MD    886-2-23123456 ext 3075    kph@ntumc.org    Principal Investigator: Ping-Hung Kuo, MD Collapse <<

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• 参考文献

• [1] Bedini A, Baiula M, Vincelli G, Formaggio F, Lombardi S, Caprini M, Spampinato S. Nociceptin/orphanin FQ antagonizes lipopolysaccharide-stimulated proliferation, migration and inflammatory signaling in human glioblastoma U87 cells. Biochem Pharmacol. 2017 Sep 15;140:89-104

  [2] Lecci A, Giuliani S, Meini S, Maggi CA. Nociceptin and the micturition reflex. Peptides. 2000 Jul;21(7):1007-21

  [3] Eto K. Nociceptin and meiosis during spermatogenesis in postnatal testes. Vitam Horm. 2015;97:167-86