antihyperalgesic

SNC 80 (NIH 10815) 是有效的，高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂，Ki 为1.78 nM，IC50 为 2.73 nM。SNC80 还以 EC50 为 52.8 nM 来选择性激活 HEK293 细胞中的 μ-δ 异聚体。SNC80 具有抗伤害性，抗痛觉过敏和抗抑郁样作用，并可用于多种头痛症的研究。

Inosine (NSC-20262) 是由腺苷分解代谢产生的一种内源性嘌呤核苷，是腺苷受体A1R 和A2AR 的激动剂，具有抗炎免疫调节，抗伤害和神经保护作用。

PD 198306 是一种具有抗痛觉过敏作用的 MAPK ERK 激酶 (MEK) 选择性抑制剂。 PD 198306 可降低链脲佐菌素诱导的活性 ERK1 水平升高。

CLP257 是有效的 K+-Cl- 协同转运蛋白 KCC2 选择性激活剂 (EC50: 616 nM)。它可减轻神经性疼痛大鼠的超敏反应，并在翻译后调节质膜 KCC2 蛋白周转。它在 KCC2 活性降低的神经元中恢复受损的 Cl- 转运。

Trimethadione (3,5,5,-Trimethyloxazolidine-2,4-dione) 是恶唑烷二酮类抗惊厥剂，也是一种 T 型钙通道阻滞剂，具有抗痛觉过敏作用，可用于研究失神发作。

1,7-Dihydroxy-2,3-methylenedioxyxanthone exhibits antiulcerogenic, anti-oxidation, and antihyperalgesic activities and can inhibit carrageenan-induced hyperalgesia.

GW405833 hydrochloride是高效选择性的大麻素-2 (CB2)受体激动剂，具有EC50值为0.65 nM和最大抑制率为44.6%。在多种啮齿动物疼痛模型中，该化合物展现了显著的镇痛效果。

Cytochrome P450 metabolism of polyunsaturated fatty acids produces numerous bioactive epoxide regioisomers. (±)10(11)-EpDPA is a docosahexaenoic acid epoxygenase metabolite, derived via epoxidation of the 10,11-double bond of DHA. It has been detected in rat brain and spinal cord, as well as human serum, and acts as a substrate for soluble epoxide hydrolase with a Km value of 5.1 μM. (±)10(11)-EpDPA and other epoxy metabolites of DHA are reported to demonstrate antihyperalgesic activity in inflammatory and neuropathic pain models and to potently inhibit angiogenesis and tumor growth in in vitro assays.

(Rac)-SNC80 是SNC80 的外消旋体。SNC80 (NIH 10815) 是一种有效的，高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂，Ki 为1.78 nM，IC50为 2.73 nM。SNC80 具有抗伤害性，抗痛觉过敏和抗抑郁样作用，并可用于多种头痛症的研究。

MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n

Cytochrome P450 metabolism of polyunsaturated fatty acids produces numerous bioactive epoxide regioisomers. (±)13(14)-EpDPA is a docosahexaenoic acid epoxygenase metabolite, derived via epoxidation of the 13,14-double bond of DHA. It has been detected in rat brain and spinal cord and is a preferred substrate for soluble epoxide hydrolase with a Km value of 3.2 μM. (±)13(14)-EpDPA demonstrates antihyperalgesic activity in inflammatory and neuropathic pain models. (±)13(14)-EpDPA and other epoxy metabolites of DHA are also reported to potently inhibit angiogenesis and tumor growth in in vitro assays.