paw

BAY-1797 是具有口服活性的选择性P2X4高效拮抗剂，对人 P2X4 的IC50为 211 nM，具有抗伤害和抗炎作用。

Taraxasteryl acetate 是分离自矢状疟原虫中，具有广谱的抗炎活性。它能够改善右旋糖酐、酵母聚糖及花生四烯酸诱导的大鼠后爪水肿。它可用于研究局部炎症。

ML-943 是选择性的、口服活性的MALT1 protease 抑制剂。它可抑制 PBMC 或全血中 IL-2 的分泌，PBMC 中抑制的IC50值为 0.07~0.09 μM，全血中抑制的IC50值为 0.6~0.8 μM)。它具有抗炎作用，可用于研究 FcgR 介导的炎症。

PAWI-2 是一种具有多重生物活性的化合物，既能激活p53，也能抑制Wnt。该化合物能抑制β3-KRAS信号传导，且此作用不依赖KRAS。PAWI-2 对TBK1的磷酸化具有选择性抑制作用，促使细胞凋亡 (Apoptosis) 通过激活caspase-3 7，并引起PARP的裂解。此外，PAWI-2 通过促进视神经素进入细胞核，导致 G2 M 停滞，并能逆转依赖于整合素β3的KRAS的人类胰腺癌干细胞 (hPCSC) 的癌症干细胞特性，同时克服耐药性。在原位异种移植小鼠模型中，PAWI-2 显著抑制 hPCSC 肿瘤的生长。

NSC15520 是一种复制蛋白 A （RPA）抑制剂，抑制 Rad9-GST 和 p53-GST 融合蛋白与 RPA N 末端 DNA 结合域 （DBD） 的结合，抑制双链 DNA （dsDNA） 寡核苷酸的螺旋不稳定，可用用于研究DNA 损伤修复。

Furaprofen 是一种可口服且具有选择性和高效性的 HCV 抑制剂，具有抗炎活性，抑制卡拉胶诱导的大鼠爪水肿，抑制较高剂量的大鼠棉粒诱导的肉芽肿。

AA 2379 是一种可口服的抗风湿剂，有抗炎和解热活性，剂量依赖性地抑制由补体介导的大鼠酵母聚糖诱导的爪水肿和小鼠酵母聚糖活化血清诱导的腹膜炎。

Zoliprofen 是一种一种高效的且可口服的非甾体抗炎剂，具有抗炎、解热和镇痛活性，对角叉菜素、制霉菌素、刀豆球蛋白A 诱导的大鼠爪水肿，以及抗大鼠兔血清诱导的骨折或背皮水肿具有抑制作用。Zoliprofen 在大鼠和兔子中对胶原蛋白或花生四烯酸引起的血小板聚集方面比布洛芬和非诺洛芬有效20倍。Zoliprofen 对小鼠内毒素诱导的腹泻和花生四烯酸诱导的兔急性死亡抑制作用显著。

Aligeron 是一种非选择性的prostaglandin (PG)拮抗剂，对PGF2α和PGE2诱导的猫血压下降有抑制作用，可用于抑制PGF2α诱导的小鼠腹泻和PGE2诱导的大鼠爪水肿。Aligeron 对血管并发症具有抗氧化保护作用。

Alnustone ((4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one) 是一种非酚双苯庚烷类化合物，在草药和香料中发现，是姜黄的成分之一，具有抗吐、抗炎作用。

7-Methoxyflavone 是一种分离自 Zornia brasiliensis 的化合物。它能够抑制福尔马林疼痛反应神经源期的舔爪时间 (65.6%)，有外周镇痛活性，但不影响炎症期的伤害性反映。

K 41498 是一种针对皮质酮释放因子受体2α（CRF2α）和CRF2β的肽拮抗剂，其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性，与CRF1相比（在表达人类受体的HEK293细胞中Ki值为425 nM）。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药，K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。

Selenomethylene blue 是一种抗氧化剂和抗炎剂，有效抑制大鼠的炎症性爪水肿。

Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg kg. 1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000)

GB 2a shows antioxidant and anti-inflammatory effects, it can prevent the carrageenan-induced paw oedema. GB 2a biflavonoid can promote inhibition on tyrosinase activity and reduced melanin biosynthesis in B16F10 cells, which suggests great potential for

Escin IIB has positive effects on acute inflammation in animals, it can inhibit the induced by serotonin in rats, the hind paw edema induced by carrageenin, and the scratching behavior induced by compound 48 80 in mice.

Boeravinone B, a novel efflux pump inhibitor, apart from inhibiting the MdeA mediated efflux, also significantly inhibit the biofilm formation of S. aureus, boeravinone B may be used in combination with mupirocin for further development. Boeravinone B exh

L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunction[2].Intrathecal injection of 30 μg of L-AP4 does not significantly alter the paw withdrawal latency in these normal rats[2].Topical application of 5 to 50 μM L-AP4 to the spinal cord significantly inhibited the evoked response of neurons to touch, pressure, pinch, and von Frey filaments in a concentration-dependent fashion[2]. Animal Model: Rats.[2] [1]. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989. [2]. Chen SR, et al. Distinct roles of group III metabotropic glutamate receptors in control of nociception and dorsal horn neurons in normal and nerve-injured Rats. J Pharmacol Exp Ther. 2005 Jan;312(1):120-6.

Arjunglucoside I has anti-inflammatory activity, it exhibits significant activity against carrageenan-induced paw edema in rat. It also shows antiproliferative activity against the A2780 human ovarian cancer cell line with an IC(50) value of 1.2 microM.

Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)

SDZ 224-015 是白细胞介素-1β（IL-1β）转化酶和 Caspase-1 的口服活性抑制剂。SDZ 224-015 具有抗 COVID-19 和抗炎活性，可减少角叉菜胶诱导的大鼠爪子水肿。

HUP-55是一种脯氨酸内肽酶的抑制剂（IC50 = 5 nM）。在10 µM的浓度下，它可减少Neuro2a细胞中α-突触核蛋白二聚体的形成，促使HEK293细胞发生自噬，并降低SH-SY5Y细胞中由过氧化氢诱导的反应性氧种（ROS）产量的增加。此外，HUP-55（10 mg kg）在通过腺病毒递送α-突触核蛋白编码载体（AAV-αSyn）诱导的帕金森病小鼠模型中，能减少患侧爪的使用和纹状体中寡聚体α-突触核蛋白水平。

Lamiide has anti-inflammatory activity in carrageenin-induced paw edema test. It shows lipid peroxidation inhibition on rat-brain phospholipid peroxidation.

Ajugasterone C shows significant inhibitory effect at 100 mg kg dose on rat paw oedema development due to carrageenan-induced inflammation in Sprague Dawley rats.