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Compound 48/80(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Compound 48/80(hydrochloride)图片
包装与价格:
包装价格(元)
50mg电议
100mg电议

产品介绍
化合物 48/80(盐酸盐)(C48/80 三盐酸盐)是 N-甲基-对-甲氧基苯乙胺与甲醛的缩合产物的混合物。

Cell lines

Bone-Marrow Derived Mast Cells

Preparation Method

Bone-Marrow Derived Mast Cells were stimulated with LPS (1 μg/ml) for 24 h and subsequently incubated with or without treatment of Compound 48/80 (50 μg/ml) for 5 min. Cells and culture supernatants were collected for the further analysis.

Reaction Conditions

Compound 48/80 (50 μg/ml);5min

Applications

Time-course analysis of dTCTP secretion by Compound 48/80 treatment demonstrated a rapid release of dTCTP within 5 min after Compound 48/80 treatment and persistent release of dTCTP during mast cell degranulation induced by Compound 48/80[1].

Animal models

Female BALB/c mice weighing 20–22 g

Preparation Method

Female BALB/c mice were randomly divided into the following 4 groups: the control, model.Thirty minutes after gavage, Compound 48/80 (0.3 mg/kg) was injected through the tail vein, and body temperature was recorded using a biological function experimental system, in which a probe was inserted into the anus of each mouse for 30 min.

Dosage form

0.3 mg/kg

Applications

In the analysis of Active Systemic Anaphylaxis, compared with the control group, the body temperature of the model group(Compound 48/80) decreased significantly.

文献引用
产品描述

Compound 48/80 trihydrochloride is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde[1].Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator[2]. Compound 48/80 was first reported in 1951 as an active histamine-releasing agent[3]that can cause redness, itching, and itching of human skin[4]. Compound 48/80 was later used as a classical mast cell activator for IgE-independent G proteins and is the most commonly used activation method in pseudoallergy studies[5]. HIS secreted by mast cells induces vasodilation, edema, pruritus, and hypothermia. Compound 48/80 trihydrochloride (C48/80 trihydrochloride) inhibits both cytosolic and particulate phosphatidylinositol-specific phospholipase C activities with a similar efficiency; IC50 values are 2.1 μg/ml (supernatant) and 5.0 μg /ml (particulate fraction). The aggregation of human platelets induced by ADP and PAF-acether is inhibited by Compound 48/80[1].Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets[6].

In vitro,Time-course analysis of dTCTP secretion by Compound 48/80 treatment demonstrated a rapid release of dTCTP within 5 min after Compound 48/80 treatment and persistent release of dTCTP during mast cell degranulation induced by Compound 48/80[7].

In vivo,In In the analysis of systemic anaphylaxis, the body temperature of the model group (Compound 48/80) was significantly lower than that of the control group. Compound 48/80 induced increased serum concentrations of HIS, TNF-α and IL-8[8]. Compound 48/80-induced MC degranulation produced anticonvulsive effects against PTZ-induced epileptic seizures by extending the onset time of both myoclonic-jerk and generalized tonic–clonic seizure, and by shortening the duration of generalized tonic–clonic seizure[9].

References:
[1]: Bronner C, Wiggins C, et,al. Compound 48/80 is a potent inhibitor of phospholipase C and a dual modulator of phospholipase A2 from human platelet. Biochim Biophys Acta. 1987 Aug 15;920(3):301-5. doi: 10.1016/0005-2760(87)90108-1. PMID: 3607084.
[2]: Schemann M, Kugler EM, et,al.The mast cell degranulator compound 48/80 directly activates neurons. PLoS One. 2012;7(12):e52104. doi: 10.1371/journal.pone.0052104. Epub 2012 Dec 18. PMID: 23272218; PMCID: PMC3525567.
[3]: Wang J, Zhang Y, et,al.Resveratrol inhibits MRGPRX2-mediated mast cell activation via Nrf2 pathway. Int Immunopharmacol. 2021 Apr;93:107426. doi: 10.1016/j.intimp.2021.107426. Epub 2021 Feb 4. PMID: 33550032.
[4]: Ding Y, Che D, et,al.Quercetin inhibits Mrgprx2-induced pseudo-allergic reaction via PLCγ-IP3R related Ca2+ fluctuations. Int Immunopharmacol. 2019 Jan;66:185-197. doi: 10.1016/j.intimp.2018.11.025. Epub 2018 Nov 21. PMID: 30471617.
[5]: Wang J, Zhang Y, et,al.Paeoniflorin inhibits MRGPRX2-mediated pseudo-allergic reaction via calcium signaling pathway. Phytother Res. 2020 Feb;34(2):401-408. doi: 10.1002/ptr.6531. Epub 2019 Oct 31. PMID: 31667930.
[6]: Kaida S, Ohta Y, Imai Y, Ohashi K, Kawanishi M. Compound 48/80 causes oxidative stress in the adrenal gland of rats through mast cell degranulation. Free Radic Res. 2010 Feb;44(2):171-80. doi: 10.3109/10715760903380466. PMID: 19886753.
[7]: Cho H, Park J, et,al. Dimerized Translationally Controlled Tumor Protein-Binding Peptide 2 Attenuates Systemic Anaphylactic Reactions Through Direct Suppression of Mast Cell Degranulation. Front Pharmacol. 2021 Oct 19;12:764321. doi: 10.3389/fphar.2021.764321. PMID: 34737708; PMCID: PMC8560797.
[8]:Zhang P, Wang Y, et,al. Allantoin Inhibits Compound 48/80-Induced Pseudoallergic Reactions In Vitro and In Vivo. Molecules. 2022 May 27;27(11):3473. doi: 10.3390/molecules27113473. PMID: 35684410; PMCID: PMC9182162. et,al.
[9]:Kilinc E, Torun IE, et,al. Mast cell activation ameliorates pentylenetetrazole-induced seizures in rats: The potential role for serotonin. Eur J Neurosci. 2022 May;55(9-10):2912-2924. doi: 10.1111/ejn.15145. Epub 2021 Feb 23. PMID: 33565644.