Application of montelukast in preparation of medicine for preventing and treating thrombotic diseases
A technology for thrombotic diseases and drugs, applied in the field of medicine, can solve the problem of not finding montelukast anti-thrombotic diseases, etc., and achieve the effects of reducing clinical trial time, preventing deep vein thrombosis, and saving research and development costs.
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Embodiment 1
[0021] Example 1: Determination of the inhibitory effect of montelukast on FXIa and its homologous serine protease activity
[0022] experimental method:
[0023] The activity of FXIa and nine homologous serine proteases was determined by the reported chemiluminescence method (Chromogenicassay), which was specifically performed in a 100 μL reaction system (containing 20 mM Tris-HCl pH 7.4, 150 mM NaCl, 0.1% BSA), FXIa or homologous serine protease at a final concentration of 10 nM was pre-incubated with montelukast at a final concentration of 0-100 μM for 15 minutes, and then a luminescent substrate (manufactured by Chromogenix, each protease at a final concentration of 200 μM) was added. The corresponding luminescent substrates are shown in Table 1), and immediately put into the BioTek Synergy 4 microplate reader after mixing, and the absorbance was detected at 405 nm, and the detection time was 30 s / read for 30 min. Each test was repeated at least 3 times. Montelukast IC w...
Embodiment 2
[0028] Embodiment 2: In vitro thrombolysis experiment of montelukast
[0029] experimental method:
[0030] Clot lysis experiments were performed in 96-well clear plates and human plasma was collected from healthy donors, collected in sodium citrate vacutainer tubes and centrifuged to obtain clear plasma. Pre-incubate 20 nM recombinant FXIa with 0-25 μM montelukast in 37 °C buffer (containing 50 mM Tris-HCl pH 7.4, 150 mM NaCl, 1% DMSO) for 15 min, then add 25% (v / v) plasma, and by immediately adding 10 mM CaCl 2 cause blood clotting. Then, the absorbance at 405 nm was measured with a microplate reader at 37° C., and the formation and dissolution of blood clots were monitored in real time. Finally, the clot coagulation curve was drawn using GraphPad Prism 5 software.
[0031] Experimental results:
[0032] Such as figure 2 As shown, the plasma in the sodium citrate vacuum blood collection tube was added with 10 mM CaCl 2After coagulation occurs, fibrin is produced and...
Embodiment 3
[0033] Example 3: Effect of Montelukast on Electrically Induced Arterial Thrombosis
[0034] experimental method:
[0035] ICR mice were randomly divided into six groups, and each group contained 6 mice. Firstly, montelukast and apixaban were administered in two gradients of 2 mg / kg and 10 mg / kg, respectively. Administration, warfarin administration dose was 4 mg / kg, normal saline administration group served as control. Three hours after administration, mice were anesthetized (1.5% pentobarbital sodium, 30 mg / kg, intraperitoneal injection) and the left common carotid artery was exposed, stimulated with a 0.1 mA current to destroy the vessel wall, thereby passing through YLS-14B animals The thrombus forming instrument forms mixed thrombus in the blood vessel, records the occlusion rate of carotid blood flow every 4 seconds through the infrared detector, and records the average time for forming occlusive thrombus in the carotid artery (occlusion rate reaches 95%).
[0036] Exp...
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