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Nocistatin

CAS No. : 207392-60-7

MCE 站：Nocistatin

产品活性：Nocistatin 是一种神经肽，是孤儿类阿片受体的内源性配体。 Nocistatin 还是神经肽伤害感受肽或孤啡肽 FQ (Noc/OFQ) 的功能性拮抗剂。Nocistatin 通过 G_i/o 蛋白介导途径抑制 5-HT 释放。Nocistatin 阻断 Nociceptin 诱导的异常性疼痛和痛觉过敏。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

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.

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.
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.
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.

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