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首页> 外文期刊>CNS drug reviews >Nitroparacetamol (NCX-701) and pain: first in a series of novel analgesics.
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Nitroparacetamol (NCX-701) and pain: first in a series of novel analgesics.

机译：硝酸对乙酰氨基酚（NCX-701）和疼痛：一系列新型镇痛药中的第一个。

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The combination of numerous classic drugs with nitric oxide donors has led to the development of new compounds with promising therapeutic activities in a great variety of situations, including cardiovascular and respiratory systems, ocular pressure, inflammation, and pain. One of the first compounds developed was NCX-701 or nitroparacetamol, resulting from the combination of paracetamol, a classic and popular analgesic used in a great number of over-the-counter medications because of its antipyretic and analgesic properties, and a nitrooxybutyroyl moiety, which releases nitric oxide at a low but steady level. Although paracetamol is devoid of most of the gastrointestinal toxicity associated with aspirin-like drugs, this type of compounds was first designed to take advantage of the cytoprotective properties of nitric oxide when released at low concentrations. However, the combination of these molecules also resulted in an unexpected enhancement of the analgesic activity of paracetamol. In fact, NCX-701 has been shown to be effective in acute nociception as well as in neuropathic pain, situations in which paracetamol and other COX inhibitors are devoid of any effect. In addition, NCX-701 is more potent and, in some circumstances, more effective than its parent compound in different models of inflammatory pain. Furthermore, whereas paracetamol lacks any effective antiinflammatory action, NCX-701 might reduce inflammation. All these results taken together imply that the mechanism of action of NCX-701 is different from that of paracetamol, although it is not yet established for either molecule. NCX-701 appears to be a promising compound in the treatment of different types of pain, with a likely better profile of side effects than its parent molecule, paracetamol. Although recent clinical trials provided data consistent with the preclinical profile of NCX-701, further studies are needed to support its clinical use.
机译：众多经典药物与一氧化氮供体的结合已导致开发出在各种情况下都具有良好治疗活性的新化合物，包括心血管和呼吸系统，眼压，炎症和疼痛。最早开发的化合物之一是NCX-701或硝基对乙酰氨基酚，它是由扑热息痛（一种由于许多种非处方药使用的经典且流行的止痛药）结合而成的，由于其具有退热和止痛作用，并带有硝基氧基丁酰基，会以较低但稳定的水平释放一氧化氮。尽管扑热息痛没有与阿司匹林样药物有关的大多数胃肠道毒性，但这类化合物首先被设计为在低浓度释放时利用一氧化氮的细胞保护特性。然而，这些分子的组合还导致扑热息痛的止痛活性出乎意料地增强。实际上，已经证明NCX-701在急性伤害感受以及神经性疼痛（对乙酰氨基酚和其他COX抑制剂没有任何作用）的情况下有效。另外，在不同的炎性疼痛模型中，NCX-701比其母体化合物更有效，在某些情况下更有效。此外，尽管扑热息痛缺乏任何有效的抗炎作用，但NCX-701可能会减轻炎症。所有这些结果加在一起表明NCX-701的作用机理与扑热息痛的机理不同，尽管这两种分子尚未确定。 NCX-701在治疗不同类型的疼痛方面似乎是一种有前途的化合物，其副作用可能比其母体对乙酰氨基酚更好。尽管最近的临床试验提供的数据与NCX-701的临床前概况相符，但仍需要进一步的研究来支持其临床应用。

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