T24692
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QAQ dichloride is a photoswitchable compound that blocks voltage-gated Na v and K v channels. Its channel-blocking activity is observed in the trans form of the azobenzene photoswitch, while the cis form does not exhibit this effect. This compound is membrane-impermeant and selectively enters pain-sensing neurons expressing endogenous import channels. QAQ dichloride functions as a light-sensitive analgesic and provides a valuable tool for investigating signaling mechanisms involved in acute and chronic pain [1] [2]. |
T61846
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CM398 is an orally active chemical compound that acts as a highly selective ligand for the sigma-2 receptor (K i =0.43 nM), demonstrating a significant ratio of selectivity between sigma-1 and sigma-2 receptors (1000-fold). Moreover, CM398 exhibits notable affinity towards dopamine (K i =32.90 nM) and serotonin transporters (K i =244.2 nM). In addition, CM398 has shown promising efficacy as an anti-inflammatory analgesic in a mouse model of inflammatory pain induced by formalin [1]. |
TP2012
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Potent, metabolically stable neurotensin receptor agonist peptide (IC50 = 0.15 nM for inhibition of [125I]-NT binding to neonatal mouse brain; EC50 = 1.9 nM for contraction of guinea pig ileum). Produces long-lasting hypothermic, neuroprotective and analg |
T73676
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MIF-1 TFA(Melanostatin)是一种内源性脑肽,具有有效调节多巴胺受体变构的作用,并抑制黑色素生成。此外,它通过阻断阿片受体的激活,调控吗啡的镇痛效果及应激诱导的镇痛(SIA)。MIF-1 TFA 能直接穿过血脑屏障(BBB)进入中枢神经系统。 |
T81117
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Spilanthol为一具有多种生物活性的化合物,包括镇痛、神经保护、抗氧化、抗诱变、抗癌、抗炎、抗菌以及杀虫作用。该化合物能够通过诱导cAMP抑制尿浓缩的负调节机制,且可作为利尿剂研究的候选物。 |
T75868
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JMV 449 acetate 是一种有效的神经降压素受体 (neurotensin receptor) 激动剂。JMV 449 acetate 显示抑制125I-neurotensin 与新生小鼠脑结合的 IC50为 0.15 nM,对收缩豚鼠回肠的 EC50为 1.9 nM。JMV 449 acetate 对小鼠具有高效、持久的降温和缓解疼痛作用。 |
T78734
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Sigma receptor
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Sigma-1 receptor antagonist 5 (compound 12) 是一种 4-吡啶衍生物,既有镇痛活性也是 sigma 受体 (Ki=4.5 nM (σ1R),10 nM (σ2R)) 及组胺 H3 (hH3R,Ki=7.7 nM,IC50=215 nM) 的拮抗剂。它能够抑制辣椒素引起的痛觉,并展现出对伤害性和神经性疼痛模型的显著疗效。 |
T78778
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Dopamine Receptor
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D3R/MOR antagonist 1 (Compound 114) 为D3R/MOR拮抗剂,其对D3R和MOR的Ki值分别为46.5 nM和691 nM。该化合物通过MOR的部分激动作用可能具有镇痛效果,同时通过D3R的拮抗作用有助于降低阿片类药物的滥用风险。 |
T79547
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Opioid Receptor
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MOR agonist-2 (Compound 46) 为D3R拮抗剂及MOR激动剂,其Ki值分别为7.26 nM和564 nM。MOR agonist-2潜在以MOR部分激动机制实现镇痛效果,并通过D3R拮抗降低阿片类药物的滥用风险。 |
T83136
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alpha-Cobratoxin 是从泰国眼镜蛇的毒液中提取的神经毒素,具有调节神经系统、抗病毒和镇痛的活性。此外,alpha-Cobratoxin 对急性及慢性多发性硬化症表现出免疫抑制作用,目前正在被进一步研究其在肾上腺脊髓神经病方面的潜在应用。 |