ptx 3

The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 μg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 μM).

ABCB1-IN-3 (Compound K27) 是一种口服活性的 ABCB1 抑制剂，能诱导细胞凋亡 (apoptosis)。该化合物直接结合 ABCB1，抑制其外排功能，确保细胞内紫杉醇 (PTX) 浓度恒定，同时不影响 ABCB1 的正常表达。在体外，ABCB1-IN-3 显著提高 ABCB1 介导的多药耐药 (MDR) 对 PTX 的敏感性，导致细胞周期停滞，抑制细胞增殖。此外，与 PTX 联合使用时，ABCB1-IN-3 在体内展现出显著的抗肿瘤活性且无毒性。