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Tritoqualine (Inhibostamin) Sale

(Synonyms: 酞茂异喹; Inhibostamin; Hypostamine) 目录号 : GC31833

Tritoqualine (Inhibostamin) 用作组氨酸脱羧酶抑制剂。

Tritoqualine (Inhibostamin) Chemical Structure

Cas No.:14504-73-5

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1mg
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

Tritoqualine (TRQ) is suspended in 0.2% Tween 80 solution[2].Male Wistar rats weighing about 150 g are used. Tritoqualine (TRQ) is given to the rats (200 mg/kg, p.o.) daily for 7 days. Hepatocytes are isolated from a perfused liver by a modified Seglen's procedure. Briefly, perfusion of the liver is started with 150 mL of a 10 mM HEPES-buffered Ca2+ free Hanks' solution (pH 7.4) containing 0.5 mM EGTA. After 5 min, the liver is excised, and the perfusate is changed to 100 mL of a recirculating HEPES-buffered Hanks' solution (pH 7.4) containing 5 mM CaCl2, 0.05% collagenase and 0.005% soybean trypsin inhibitor instead of EGTA. The process continues for 15-20 min at 37°C with aeration of carbogen (95% O2, 5% CO2), until the liver began to disintegrate visibly. Cells are dispersed in a HEPES-buffered Hanks' solution (pH 7.4), filtered through a nylon stocking, and sedimented by triple centrifugation for 1 min at 50×g. Finally, the hepatocytes are suspended at 5×105 cells/mL in the same solution supplemented with 2% BSA. Two mL of the cell suspension is placed on 35 mm diameter culture dishes and incubated in an incubator at 37 °C. CCl4 is diluted with ethanol (10%, v/v) and added to the dishes at a concentration of 2.6 or 5.2 mM (0.25 or 0.5%, v/v, respectively). As a marker of cell membrane damage, lactate dehydrogenase (LDH) leaked out from the cells is determined using the supernatant of centrifuged samples. Total LDH activity is measured after lysis of the cells by sonication. The results are expressed as a ratio of LDH release induced by CCl4 to total LDH in the cells[2].

Animal experiment:

Rats[2] Tritoqualine (TRQ) is given p.o. to rats weighing about 200 g daily for 14 days. The same amount of 0.2% Tween 80 solution is given to the other rats. CCl4 diluted with olive oil (37.5%, v/v) is given to the rats (0.75 mL/kg, i.p.) 4 hr after the last administration of these compounds. The animals are killed 20 hr after the injection of CCl4. Serum is obtained from arterial blood. The liver is washed with 1.15% KCl solution through the portal vein, excised and homogenized in ten volumes of the same solution. Lipid peroxidation in the liver homogenates is quantified by the 1 % phosphoric acid method. All manipulations are done rapidly on ice to avoid further peroxidation. Glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) in the serum are measured using commercial test kits.

References:

[1]. Ishii K, et al. Therapeutic effect of histidine decarboxylase inhibitor on chronic active hepatitis. Gastroenterol Jpn. 1978;13(2):105-10.
[2]. Yuasa S, et al. Suppressive effect of tritoqualine on lipid peroxidation and enzyme leakage induced by carbon tetrachloride in rat hepatocytes. Jpn J Pharmacol. 1986 Jun;41(2):205-10.

产品描述

Tritoqualine is used as a histidine decarboxylase inhibitor.

The effect of Tritoqualine (TRQ) on the CCl4-induced enzyme leakage is investigated by pretreatment of rats with Tritoqualine (200 mg/kg/day, p.o., 7 days). The ratio of lactate dehydrogenase (LDH) release from the cells of Tritoqualine-pretreated rats is significantly less than that in control rats. The rate of malondialdehyde (MDA) production is accelerated after the addition of 7.8 mM CCl4. Tritoqualine reduces its rate in a dose dependent manner, and it completely prevents CCl4-stimulated lipid peroxidation at a concentration of 33 μM[2].

A single administration of CCl4 (0.75 mL/kg, p.o.) causes a five-fold increase of in vivo lipid peroxidation in the liver. In contrast, a reduction of 37% in the lipid peroxidation is obtained by Tritoqualine (100 mg/kg) pretreatment for 14 days prior to CCl4 treatment. A 63% reduction is observed in vitamin E (25 mg/kg) pretreated rats[2].

[1]. Ishii K, et al. Therapeutic effect of histidine decarboxylase inhibitor on chronic active hepatitis. Gastroenterol Jpn. 1978;13(2):105-10. [2]. Yuasa S, et al. Suppressive effect of tritoqualine on lipid peroxidation and enzyme leakage induced by carbon tetrachloride in rat hepatocytes. Jpn J Pharmacol. 1986 Jun;41(2):205-10.

Chemical Properties

Cas No. 14504-73-5 SDF
别名 酞茂异喹; Inhibostamin; Hypostamine
Canonical SMILES O=C1OC(C2N(C)CCC3=C2C(OC)=C(OCO4)C4=C3)C5=C1C(N)=C(OCC)C(OCC)=C5OCC
分子式 C26H32N2O8 分子量 500.54
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9978 mL 9.9892 mL 19.9784 mL
5 mM 0.3996 mL 1.9978 mL 3.9957 mL
10 mM 0.1998 mL 0.9989 mL 1.9978 mL
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Research Update

[Hypostamine (tritoqualine), a synthetic reference antihistaminic]

The role of histamine in hypersensitivity reactions justifies the use of antagonistic medication. The symptomatic action of the antihistamines has led many workers to forget the role of the drug in reducing histamine (hypohistaminic), in which interest should remain as a curative and mainly preventive medication. The main indications for the action of this drug at the level of physiopathological mechanism involved are: disorders that implicate the production of endogenous histamine, prevention of histamine release, reduction of over-production of histamine by regulation of receptor saturation, symptomatic action without side effects.

[Effect of tritoqualine on the histamine levels of whole blood]

For ten years now, tritoqualine, a histidine decarboxylase inhibitor, has been advocated in a prevention protocol for anaphylactoid reactions occurring during general anaesthesia. The present double-blind study aimed to quantify the effects of the drug on whole blood histamine levels. 44 patients were assigned at random to two different groups, one taking 300 mg t.i.d. tritoqualine for three days, and the other taking a placebo. The histamine levels were measured before the treatment and 12 h after the last dose of the drug after haemolysis of the sample, by the fluorometric technique preceded by column chromatography. In the group taking tritoqualine, the histamine level fell from a mean of 109 +/- 61 to 91 +/- 41 ng X ml-1, whereas it rose from a mean of 92 +/- 55 to 105 +/- 62 ng X ml-1 in the control group taking placebo. These variations were not statistically significant. In both groups were present four volunteers with a history of allergy; their histamine level fell from 107 +/- 35 to 71 +/- 36 ng X ml-1 after tritoqualine intake (p less than 0.05), whereas it rose from 76 +/- 19 to 162 +/- 36 ng X ml-1 after placebo (p less than 0.05). The small differences found in the whole blood histamine level 12 h after the last oral dose of the drug suggested that the present tritoqualine dose regimen was inadequate to achieve the aims of its prescription.

Clinical pharmacology of tritoqualine: a comparative study against dexchlorpheniramine in allergic rhinitis

The effect of tritoqualine on seasonal allergic rhinitis caused by grass pollen was compared to that of dexchlorpheniramine maleate (DCPM) in 21 patients randomly allocated into two parallel groups. There were rapid improvements of all symptoms considered after treatment with either tritoqualine or DCPM. A significant reduction of plasma histamine concentrations was observed during the treatment with tritoqualine whereas no modification occurred with DCPM. Finally, it was shown that tritoqualine did not modify reaction times to visual and auditive stimuli whereas DCPM induced a significant slowing-down of the reaction time to visual stimuli. From this pilot study tritoqualine appears to have the same efficacy for the treatment of seasonal allergic rhinitis as classic anti-H1 antihistamines, but without central nervous system side-effects.

Inhibitory mechanism of tritoqualine on histamine release from mast cells

Tritoqualine (TRQ, (+)-(R*)-7-amino-4,5,6-triethoxy-3-[(R*)-5,6,7, 8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin++ +-5-yl] phthalide) strongly inhibited the increased metabolism of [3H]arachidonic acid-labeled phospholipid and 45Ca2+ influx in mast cells stimulated by compound 48/80 (compd 48/80), Concanavalin A (Con A) plus phosphatidylserine (PS), or 2,4-dinitrophenyl-coupled-ascaris extracts (DNP-asc). However, TRQ did not disturb the binding of 14C-labeled compd 48/80 to the mast cell membrane. The activity of calmodulin purified from mastocytoma P-815 cells was inhibited by TRQ at IC50 1.0 microM. From these results, it is concluded that the inhibitory mechanism of TRQ on stimulus-induced histamine release from mast cells may be mediated at least partially by the inhibition of Ca2+ influx and calmodulin activity.

Is histamine involved in ethanol-induced inflammation?

The participation of histamine in ethanol-induced inflammation has been estimated in rats. Administration of ethanol caused an increase in the total number of blood leukocytes and changed the composition of the leukocyte population. The histamine receptor antagonists mepyramine and cimetidine did not affect the changes in cellular composition. Pretreatment with the anti-allergic drug Tritoqualine had no effect on the total number of leukocytes and PMN-leukocytes. PMN-leukocytes from ethanol treated rats had a greater capacity to activate latent collagenase. This ability was partially inhibited by the histamine receptor antagonists mepyramine and cimetidine, particularly in combination. Pretreatment with Tritoqualine apparently protected the latent collagenase against ethanol activation. Thus we conclude that histamine is possibly implicated in the process of generating activity for latent collagenase.