Thiazinamium chloride (Multergan chloride)
目录号 : GC31807Thiazinamiumchloride化物具有有效的抗胆碱和抗过敏活性,并抑制TxB2合成其IC50值为0.2µM。
Cas No.:4320-13-2
Sample solution is provided at 25 µL, 10mM.
Thiazinamium chloride possesses potent anticholinergic and antiallergic activity and inhibits TxB2 synthesis with IC50 value of 0.2 µM.
TxB2 synthesis by resting macrophages is inhibited by thiazinamium chloride and promethazine in a dose-dependent manner. Thiazinamium chloride inhibits TxBz synthesis but had no effect on the ingestion of zymosan particles. In contrast, chlorpromazine inhibits phagocytosis but not TxBz synthesis except at lo-3 M. Under the condition where indomethacin, a nown cyclooxygenase inhibitor, is inhibitory, promethazine but not thiazinamium chloride inhibits TxB2 synthesis from exogenous arachidonic acid. Treatment of macrophages with promethazine and chlorpromazine but not thiazinamium chloride results in a reduction in the oxidative burst during phagocytosis. Furthermore, the ability of thiazinamium chloride to selectively inhibit arachidonic acid metabolism may contribute to its bronchodilator/antiallergic activity[1].
[1]. Chang J, et al. Effects of thiazinamium chloride, promethazine and chlorpromazine on thromboxane B2 synthesis, phagocytosis and respiratory burst by rat alveolar macrophages. Biochem Pharmacol. 1983 Sep 15;32(18):2671-7.
Cell experiment: | Rats are anesthetized with an intraperitoneal injections of sodium pentobarbital (43mg/kg body wt) and exsanguinated by cardiac puncture; their lungs are isolated and lavaged with a total of 50mL of lavage solution. Lungs that exhibit infection or gross pathological changes are not used. The lavage fluid containing macrophages is centrifuged at 300g for 10 min, and the cell pellet is resuspended in serum free M199. Macrophage monolayers are established by incubating 1.5x106 cells in petri dishes (35x10mm) for 2 hr in an atmosphere of 95% room air and 5% carbon dioxide. After washing with I-IBSS to remove non-adherent cells, the cultures are incubated in serum-free Ml99 with or without zymosan (100μg/mL) in the absence or presence of drugs(including Thiazinamium chloride)[1]. |
References: [1]. Chang J, et al. Effects of thiazinamium chloride, promethazine and chlorpromazine on thromboxane B2 synthesis, phagocytosis and respiratory burst by rat alveolar macrophages. Biochem Pharmacol. 1983 Sep 15;32(18):2671-7. |
Cas No. | 4320-13-2 | SDF | |
Canonical SMILES | C[N+](C)(C)C(C)CN1C2=C(C=CC=C2)SC3=CC=CC=C13.[Cl-] | ||
分子式 | C18H23ClN2S | 分子量 | 334.91 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.9859 mL | 14.9294 mL | 29.8588 mL |
5 mM | 0.5972 mL | 2.9859 mL | 5.9718 mL |
10 mM | 0.2986 mL | 1.4929 mL | 2.9859 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
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