Muscle relaxation accelerator and therapeutic agent for muscular tissue diseases such as muscle relaxation failure
A kind of heart failure, myocardial technology, applied in the treatment or prevention of intramyocardial microvascular angina pectoris, angina pectoris, treatment or prevention of heart failure, treatment or prevention of acute pulmonary edema, treatment of catecholamine-induced arrhythmia Drugs or preventive drugs, active compounds, therapeutic drugs for hypertension, diseases related to myocardial diastolic disorders, therapeutic drugs for catecholamine-induced hypertension, can solve problems such as the prevention of sudden death, coronary perfusion disorder, and reduction of blood drug concentration by meta-method
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experiment example 1
[0056] In this example, the above-mentioned 1,4 benzothiazepine The pharmaceutically acceptable salt of the derivative uses the monohydrochloride of this compound, i.e. 4-[3-(4-benzylpiperidin-1-yl) propionyl]-7-methoxy-2,3,4, 5-tetrahydro-1,4-benzothiazepine The monohydrochloride (hereinafter referred to as the present compound). Wistar male rats, 8 weeks old and weighing 300-330 g, were used. Anesthesia was performed by subperitoneal injection of 1000 mg / kg urethane and 80 mg / kg α-chloralose, and natural respiration was used. In this example, 100 mg of the present compound was dissolved in 1 mL of dimethyl sulfoxide (DMSO) to prepare a DMSO solution of the present compound, and the solution was stored at 4°C. The injection amount of norepinephrine is 40 μg / kg / min, and its preparation method is to dissolve 1 mg of norepinephrine in 41 μL of distilled water to make a norepinephrine solution.
[0057] First, a cannula for continuous infusion of calcium chloride aqueous so...
experiment example 2
[0069] The effect of this compound on blood pressure
[0070] In this experiment, 8-week-old wistar male rats weighing 310 and 330 g were used. Anesthesia was performed by subperitoneal injection of 1000 mg / kg urethane and 80 mg / kg α-chloralose, and natural respiration was used. In this experimental example, 100 mg of the present compound was dissolved in 1 mL of dimethyl sulfoxide (DMSO) to prepare a DMSO solution of the present compound, and the solution was stored at 4°C. Separately, 1 mg of norepinephrine was dissolved in 41 μL of distilled water to prepare a norepinephrine solution.
[0071] This example was carried out at a room temperature of 20-25° C. as in the above-mentioned Experimental Example 1. This example is also the same as the above-mentioned Experimental Example 1. The cannula that continuously injects calcium chloride aqueous solution or norepinephrine aqueous solution containing calcium chloride is inserted into the right external jugular vein of the abo...
experiment example 3
[0083] Study on the effect of the compound on the diastolic ability of the left ventricular wall by tissue Doppler method
[0084] In this experimental example, 9-week-old Wistar male rats with body weights of 310 and 320 g were used. Anesthesia was performed by subperitoneal injection of 1000 mg / kg urethane and 80 mg / kg α-chloralose, and natural respiration was used. In this experimental example, 100 mg of the present compound was dissolved in 1 mL of dimethyl sulfoxide (DMSO) to prepare a DMSO solution of the present compound, and the solution was stored at 4°C. Separately, 1 mg of norepinephrine was dissolved in 41 μL of distilled water to prepare a norepinephrine solution.
[0085] This example was carried out at a room temperature of 20-25° C. as in the above-mentioned Experimental Example 1. This example is also the same as the above-mentioned Experimental Example 1. A cannula that continuously injects calcium chloride aqueous solution or norepinephrine aqueous solutio...
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