Nocistatin 

Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia^[1][2]. In Vitro:In the isolated organ bath studies Nocistatin (1 pM-1μM) inhibits the prostaglandin- and the KCl-evoked contractions in the uterus dose-dependently. Nocistatin, generated locally in the uterus, exerts an inhibitory effect, the mechanism being mediated in part by Ca²⁺-dependent K⁺ channels, the elevation of cAMP levels and sensory neuropeptides^[1].
In Vivo:Intrathecal administration of Nocistatin (10 pg-1 μg) nociceptin or orphanin FQ (Noc/OFQ) induces pain responses including allodynia and hyperalgesia. Simultaneous administration of Nocistatin blocks the allodynia and hyperalgesia induced by Noc/OFQ^[2].
Nocistatin also attenuates the allodynia and hyperalgesia evoked by prostaglandin E2 and the inflammatory hyperalgesia induced by formalin or carrageenan/kaolin, and reversed the Noc/OFQ-induced inhibition of morphine analgesia at picogram doses^[2].
Nocistatin counteracted the impairment of learning and memory induced by Noc/OFQ or scopolamine. Nocistatin is widely present in the spinal cord and brain. Although Nocistatin does not bind to the Noc/OFQ receptor, it binds to the membrane of mouse brain and spinal cord with a high affinity^[2].

772.85

C₃₂H₅₆N₁₀O₁₂

207392-60-7

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• [1]. Beáta H Deák, et al. Nocistatin inhibits pregnant rat uterine contractions in vitro: roles of calcitonin gene-related peptide and calcium-dependent potassium channel. Eur J Pharmacol. 2013 Aug 15;714(1-3):96-104.  [Content Brief]

  [2]. E Okuda-Ashitaka, et al. Nocistatin: a novel neuropeptide encoded by the gene for the nociceptin/orphanin FQ precursor. Peptides. 2000 Jul;21(7):1101-9.  [Content Brief]