BzATP triethylammonium salt is a potent adenosine triphosphate (ATP) analog that primarily acts as a purinergic P2X receptor (EC50：rat P2X7 = 3.6μM；mouse P2X7 = 285μM) [1]. BzATP triethylammonium salt activates the P2X7 receptor, opening nonselective cation channels on the cell membrane [2]. BzATP triethylammonium salt promotes Ca2⁺ and Na⁺ influx and K⁺ efflux, thereby inducing a cellular inflammatory signaling cascade, including NLRP3 inflammasome activation and the release of inflammatory cytokines such as IL-1β and IL-18 [3]. BzATP triethylammonium salt is commonly used to study physiological and pathological processes such as neuroinflammation, immunoregulation, and apoptosis [4].
In U87 glioma cells, BzATP triethylammonium salt (5-1000μM; 72h) promotes glioma cell proliferation by activating P2X7 receptors, leading to significantly enhanced cell activity and proliferation [5]. In A549 cells, BzATP triethylammonium salt (150-600μM; 72h) can inhibit cell proliferation and induce apoptosis, and its mechanism of action may be associated with promoting the release of TNF-α and inhibiting the NF-κB signaling pathway [6].
In 4T1 cells breast cancer-bearing mice model, BzATP triethylammonium salt (50μg/kg; ip; 7d) treatment significantly increased tumor weight, myeloid lymphocyte infiltration, and P2X7 expression at the protein and cellular levels [7]. In collagen-induced arthritis (CIA) mice model, BzATP triethylammonium salt (1mg/kg; ip; 20d) treatment restored the damaging effects of erastin and alleviated metabolic abnormalities [8].
References:
[1]. Bianchi B R, Lynch K J, Touma E, et al. Pharmacological characterization of recombinant human and rat P2X receptor subtypes[J]. European journal of pharmacology, 1999, 376(1-2): 127-138.
[2]. Young M T, Pelegrin P, Surprenant A. Amino acid residues in the P2X7 receptor that mediate differential sensitivity to ATP and BzATP[J]. Molecular pharmacology, 2007, 71(1): 92-100.
[3]. Anderson A, Waithe O Y, Seplovich G, et al. Regulation of BzATP‐Induced Blood–Brain Barrier Endothelial Cell Hyperpermeability by NLRP3 Inflammasome Inhibition[J]. Microcirculation, 2025, 32(3): e70006.
[4]. Shieh C H. The role of purinergic receptors in the regulation of mRNA expression and release of inflammatory cytokines in cultured primary mouse glia[D]. Dissertation, Universität Freiburg, 2014, 2014.
[5]. Ji Z, Xie Y, Guan Y, et al. Involvement of P2X7 receptor in proliferation and migration of human glioma cells[J]. BioMed research international, 2018, 2018(1): 8591397.
[6]. ZENG K, RU Q, XIONG Q, et al. Effect of P2X7R agonist BzATP on cell growth and apoptosis in non-small cell lung cancer A549 cells[J]. Journal of International Oncology, 2016: 321-325.
[7]. Yu X, Chen X, Tang X, et al. P2X7 blockade inhibits the growth of breast cancer in 4T1 breast cancer-bearing mice by NLRP3/caspase 1 pathway[J]. Archives of Medical Science, 2020, 16(1).
[8]. Ma Y, Li W, Niu S, et al. BzATP reverses ferroptosis-induced gut microbiota disorders in collagen-induced arthritis mice[J]. International Immunopharmacology, 2023, 124: 110885.
BzATP triethylammonium salt是一种强效的三磷酸腺苷（ATP）类似物，主要作为嘌呤能P2X受体发挥作用（EC50：大鼠P2X7 = 3.6μM；小鼠P2X7 = 285μM) [1]。BzATP triethylammonium salt可激活P2X7受体，打开细胞膜上的非选择性阳离子通道 [2]。BzATP triethylammonium salt促进Ca2⁺和Na⁺内流以及K⁺外流，从而诱导细胞炎症信号级联，包括NLRP3炎症小体激活和炎症细胞因子（如IL-1β和IL-18）的释放 [3]。BzATP triethylammonium salt常用于研究神经炎症、免疫调节和细胞凋亡等生理和病理过程 [4]。
在U87胶质瘤细胞中，BzATP triethylammonium salt（5-1000μM；72h）通过激活P2X7受体促进胶质瘤细胞增殖，导致细胞活性和增殖能力显著增强 [5]。在A549细胞中，BzATP triethylammonium salt（150-600μM；72h）能抑制细胞增殖、诱导细胞凋亡，其作用机制可能与促进TNF-α的释放、抑制NF-κB信号通路有关 [6]。
在4T1细胞乳腺癌荷瘤小鼠模型中，BzATP triethylammonium salt（50μg/kg；ip；7d）治疗在蛋白和细胞水平上显著增加肿瘤重量、髓系淋巴细胞浸润以及P2X7的表达 [7]。在胶原导性关节炎（CIA）小鼠模型中，BzATP triethylammonium salt（1mg/kg；ip；20d）治疗可恢复erastin的破坏作用并减轻代谢异常 [8]。