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Inflammatory Pain Pharmacological Treatment Strategy with Prostaglandin E Receptor 4 Antagonist

机译:前列腺素E受体4拮抗剂的炎性疼痛药理治疗策略

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Prostaglandin E2 (PGE2) has been associated with inflammatory conditions and is considered a proinflammatory mediator in the mechanism of inflammation and pain hypersensitivity. PGE2 is a major mediator of peripheral inflammation and processing of pain signals. Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly applied as the pain reliever attempts to inhibit COX-1 and/or COX-2 to lessen occurrence of PGE2 and other prostanoids. However, usage of COX inhibitors has been reported to have side effects that include gastrointestinal and renal toxicity, and certain types of COX-2 inhibitors are associated with an increased cardiovascular risk among patients. In view of this, an alternative strategy by target PGE2 production with inhibitors of PGE synthases or blockade of PGE2 receptors was suggested to develop analgesics that enable prevention of potential cardiovascular and renal side-effects.
机译:前列腺素E2(PGE2)与炎症有关,被认为是炎症和疼痛超敏反应机制中的促炎介质。 PGE 2是周围炎症和疼痛信号处理的主要介质。非甾体类抗炎药(NSAIDs)通常用于缓解疼痛的药物中,试图抑制COX-1和/或COX-2以减少PGE2和其他类前列腺素的发生。然而,据报道,使用COX抑制剂具有包括胃肠道和肾脏毒性在内的副作用,并且某些类型的COX-2抑制剂会增加患者的心血管风险。有鉴于此,有人提出了通过用PGE合成酶抑制剂或PGE2受体阻断来产生靶PGE2的替代策略,以开发止痛药,以预防潜在的心血管和肾脏副作用。

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    《Inside R & D》 |2013年第10期|3-4|共2页
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