Oxatomide是一种口服活性的H1受体拮抗剂（抗组胺药）。
Cas No.:60607-34-3
Sample solution is provided at 25 µL, 10mM.
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Oxatomide is an orally active H1-receptor antagonist (antihistamine)[1-2]. Oxatomide is used in the treatment of allergic diseases such as allergic rhinitis, urticaria, and conjunctivitis[3-4].
In vitro, Oxatomide (1-10µM) was incubated with P-glycoprotein-expressing doxorubicin-resistant human leukemia K562/DXR cells for 45 minutes. Oxatomide significantly reversed the multidrug resistance phenotype in K562 cells and increased the intracellular accumulation of chemotherapeutic drugs[5]. Oxatomide (0.1–30µM) was used to pretreat mouse neuroblastoma N18TG2 cells, J774 macrophage cells, human myeloma RPMI8226 cells, and mouse bone marrow-derived mast cells (mBMMC) expressing functional P2X7 receptors for 1 minute, followed by stimulation with ATP (0.5–3mM) or BzATP (10–100µM). Oxatomide significantly inhibited P2X7 receptor-mediated calcium influx, membrane currents, mitogen-activated protein kinase (MAPK) activation, induction of inflammation-related genes, cell death (as measured by LDH release), and mast cell degranulation[6].
In vivo, Oxatomide (1.25–5mg/kg) was orally administered 4 hours prior to challenge to sensitized male Swiss strain mice that had been infected with Trichinella spiralisfor 30 to 40 days. Oxatomide dose-dependently and significantly prevented a lethal anaphylactic reaction induced by intravenous injection of Trichinella larval somatic antigens[7]. Oxatomide (100mg/kg) was administered as a single oral dose 30 minutes before the antigen challenge to passively sensitized WBB6F1-+/+ and B6D2F1 mice using a high dilution (1:128) of anti-bovine serum albumin (BSA) serum. Oxatomide inhibited the passive cutaneous anaphylaxis (PCA) reaction triggered by the high-dilution antiserum[8].
References:
[1] Hayashi K, Yanagi M, Wood-Baker R, et al. Oxatomide for stable asthma in adults and children. Cochrane Database Syst Rev. 2003;2003(2):CD002179.
[2] Richards DM, Brogden RN, Heel RC, et al. Oxatomide. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Mar;27(3):210-31.
[3] Marone G, Granata F, Spadaro G, et al. Antiinflammatory effects of oxatomide. J Investig Allergol Clin Immunol. 1999 Jul-Aug;9(4):207-14.
[4] Yamagiwa N, Komine M, Hanaoka F, et al. Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity. Bioorg Med Chem Lett. 2022 Dec 1;77:129035.
[5] Ishikawa M, Fujita R, Furusawa S, et al. Circumvention of acquired resistance to doxorubicin in K562 human leukemia cells by oxatomide. Biol Pharm Bull. 2001 Oct;24(10):1185-7.
[6] Yoshida K, Ito M, Matsuoka I. P2X7 receptor antagonist activity of the anti-allergic agent oxatomide. Eur J Pharmacol. 2015 Nov 15;767:41-51.
[7] De Clerck F, Van Gorp L, Vanparijs O, et al. Oxatomide protects Trichinella spiralis infected mice from lethal anaphylaxis. Agents Actions. 1978 Dec;8(6):568-71.
[8] Kimura S, Watanabe A, Takeuchi M, et al, Drug susceptibility of PCA in WBB6F1-W/Wv mice. Cell Mol Life Sci. 1998 May;54(5):456-60.
Oxatomide是一种口服活性的H1受体拮抗剂（抗组胺药）[1-2]。Oxatomide可用于过敏性鼻炎、荨麻疹和结膜炎等过敏性疾病的治疗[3-4]。
在体外，Oxatomide（1-10μM）处理表达P-糖蛋白的阿霉素耐药人白血病细胞K562/DXR 45分钟。Oxatomide可显著逆转K562细胞多药耐药表型，同时增加细胞内化疗药物的积累[5]。Oxatomide（0.1–30μM）预处理表达功能性P2X7受体的小鼠神经母细胞瘤N18TG2细胞、J774巨噬细胞、人骨髓瘤RPMI8226细胞及小鼠骨髓来源肥大细胞（mBMMC）1分钟，随后以ATP（0.5–3mM）或BzATP（10–100μM）刺激。Oxatomide显著抑制P2X7受体介导的钙离子内流、膜电流、丝裂原活化蛋白激酶（MAPK）激活、炎症相关基因诱导、细胞死亡（LDH释放）及肥大细胞脱颗粒[6]。
在体内，Oxatomide（1.25–5mg/kg）在攻击前4小时经口给药，用于处理经旋毛虫（Trichinella spiralis）感染30至40天、处于致敏状态的瑞士品系雄性小鼠。Oxatomide呈剂量依赖性显著防止了由静脉注射旋毛虫幼虫体抗原引发的致死性过敏反应[7]。Oxatomide（100mg/kg）在抗原攻击前30分钟单次给药（口服），用于处理经高稀释度（1:128）抗牛血清白蛋白（BSA）血清被动致敏的WBB6F1-+/+和B6D2F1小鼠。Oxatomide抑制了由高稀释度抗血清引发的被动皮肤过敏反应（PCA）[8]。
| Cell experiment [1]: | |
Cell lines | K562 human leukemia cells and K562 doxorubicin-resistant variant K562/DXR |
Preparation Method | K562 and K562/DXR cells were maintained in RPMI 1640 medium supplemented with 10% fetal calf serum. The K562/DXR cell line was maintained in medium containing 1μM doxorubicin, which was washed out at least 3 days before experiments. For cytotoxicity assays, cells were incubated with various concentrations of Oxatomide (1–10μM; 45min) and doxorubicin. |
Reaction Conditions | 11–10μM; 45min. |
Applications | Oxatomide synergistically and dose-dependently potentiated the cytotoxicity of doxorubicin in P-glycoprotein-expressing K562/DXR cells but not in the parental K562 cells. Oxatomide significantly increased the intracellular accumulation of doxorubicin in K562/DXR cells and inhibited the photolabeling of P-glycoprotein by [³H]-azidopine, indicating direct interaction with and inhibition of the P-glycoprotein drug-efflux pump. |
| Animal experiment [2]: | |
Animal models | Mast cell-bearing WBB6F1-+/+ mice and B6D2F1 mice |
Preparation Method | 30 minutes after the mice were given the Oxatomide (100mg/kg) orally, shaved on the dorsal skin and intradermally injected with a high dilution (1:128 or 1:256) of hyperimmune anti-bovine serum albumin (anti-BSA) serum to passively sensitize the skin for IgG1 antibody-mediated passive cutaneous anaphylaxis (PCA). One hour later, PCA was elicited by an intravenous injection of BSA antigen mixed with Evans blue dye. |
Dosage form | 100mg/kg; p.o.; single administration 30 minutes before the antigen challenge |
Applications | Oxatomide nearly completely suppressed the IgG1 antibody-mediated passive cutaneous anaphylaxis (PCA) reaction in mast cell-bearing reference mice, as indicated by a significant reduction in the amount of dye extravasated at the skin reaction site. |
References: | |
| Cas No. | 60607-34-3 | SDF | |
| 别名 | 欧诗美锭 | ||
| Canonical SMILES | O=C1NC2=CC=CC=C2N1CCCN3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3 | ||
| 分子式 | C27H30N4O | 分子量 | 426.55 |
| 溶解度 | DMSO: 250 mg/mL (586.10 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3444 mL | 11.722 mL | 23.4439 mL |
| 5 mM | 468.9 μL | 2.3444 mL | 4.6888 mL |
| 10 mM | 234.4 μL | 1.1722 mL | 2.3444 mL |
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