目录号 | 产品详情 | 靶点 | |
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T40045 | P2X Receptor | ||
Sivopixant (S-600918) 是P2X3受体选择性拮抗剂 (P2X3IC50=4.2 nM; P2X2/3IC50=1100 nM)。Sivopixant 可用于缓解疼痛的研究。 | |||
T1431 | EGFR Others | ||
Khellin (Methafrone) 是从阿米芹中提取得到的一种呋喃并色酮,是EGFR 抑制剂,IC50为 0.15 µM。它体外具有抗增殖活性,还具有抗痉挛和冠状动脉舒张作用。 | |||
T1191L | COX | ||
Metamizole sodium (Analgin) 是一种环氧合酶-3 (COX-3) 抑制剂,具有良好的解热作用,可用于缓解疼痛的研究。 | |||
T2367 | p38 MAPK TNF | ||
SKF-86002 是一种可口服的 p38 MAPK 抑制剂,具有抗炎和抗关节炎活性,可用于缓解疼痛的研究。它能抑制脂氧合酶和环氧合酶介导的花生四烯酸代谢,还抑制脂多糖 (LPS) 刺激人单核细胞产生 IL-1 和 TNF-α,IC50为 1 μM。 | |||
T1115 | Histamine Receptor | ||
Doxylamine succinate (Decapryn) 是一种吡啶衍生物组胺 H1 拮抗剂,具有明显的镇静特性。它竞争性阻断组胺 H1 受体并限制典型的过敏和过敏反应,可防止组胺引起的皮肤和粘膜疼痛和瘙痒。 | |||
T0463 | COX | ||
Loxoprofen (Koloxo) 是一种非甾体类抗炎药,具有解热作用,可用于缓解疼痛的研究。它是非选择性COX 抑制剂,对 COX-1 和 COX-2 的IC50分别为 6.5 和 13.5 μM。 | |||
T0456 | COX | ||
Cinchophen (Cinconal) 是口服具有活性的非甾体抗炎试剂,具有抗菌活性。它可用于研究关节炎和某些肝脏疾病。 | |||
T4351 | Opioid Receptor | ||
DAMGO (DAGO) 是一种阿片受体激动剂,Kd 值为 3.46 nM。它能够影响啮齿动物的运动活动,可作为镇痛剂。 | |||
T3S0870 | ATPase Potassium Channel NO Synthase | ||
Paederosidic acid methyl ester 是 ATP 敏感的 K+channel 通道激活剂,分离自 P. scandens。它通过激活脑中和脊髓水平中 ATP 敏感型 K+通道提高了痛觉阈值,表现出显著的中枢缓解疼痛活性。 | |||
T9833 | P2X Receptor GlyT 5-HT Receptor | ||
Opiranserin hydrochloride 是甘氨酸转运蛋白 2 型 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂,IC50 分别为 0.86 和 1.3 μM。它显示对 rP2X3 的拮抗活性 (IC50=0.87 μM)。它正在开发为用于治疗术后疼痛的注射剂。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-00055 | Alpha-toxin Amm8 Protein, Androctonus mauritanicus, Recombinant (His & Myc) | Androctonus mauritanicus | Baculovirus | ||
Alpha toxins bind voltage-independently at site-3 of sodium channels (Nav) and inhibit the inactivation of the activated channels, thereby blocking neuronal transmission. The toxin principally slows the inactivation process of TTX-sensitive sodium channels. It discriminates neuronal versus muscular sodium channel, as it is more potent on rat brain Nav1.2/SCN2A (EC(50)=29 nM) than on rat skeletal muscle Nav1.4/SCN4A (EC(50)=416 nM). It also shows a weak activity on Nav1.7/SCN9A (EC(50)=1.76 uM). In vivo, the toxin produces pain hypersensibility to mechanical and thermal stimuli.(PubMed:23685008). It also exhibits potent analgesic activity (when injected intraperitoneally), increasing hot plate and tail flick withdrawal latencies in a dose-dependent fashion. This paradoxical analgesic action, is significantly suppressed by opioid receptor antagonists, suggesting a pain-induced analgesia mechanism that involves an endogenous opioid system. This led to hypothesis that pain relief induced by peripheral administration of Amm VIII may result from sensitization of primary afferent neurons and subsequent activation of an opioid-dependent noxious inhibitory control.
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