Oxatomide |
رقم الكتالوجGC61401
One-Click Copy Product Info
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Oxatomide هو مستقبلات الهيستامين المزدوجة القوية والفعالة عن طريق الفم ومضاد مستقبلات P2X7 مع نشاط مضاد للهستامين ومضاد للحساسية
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Canonical SMILES | O=C1NC2=CC=CC=C2N1CCCN3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3 | ||
| Formula | C27H30N4O | M.Wt | 426.55 |
| الذوبان | DMSO: 250 mg/mL (586.10 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)