Tropodifene (Tropaphen)
(Synonyms: 托泊地芬,Tropaphen) 目录号 : GC32642
Tropodifene (Tropaphen) (Tropaphen) 是一种 α-Adrenergic receptor 抑制剂。
Cas No.:15790-02-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rabbits[1]The drug is injected intravenously into rabbits. Experiments on the isolated ears of the rabbits are carried out by the Kravkov--Pisemskii method. The effect of tropaphen on the ear vessels of the intact rabbit is judged by the changes in the temperature of the ear. The temperature is measured by means of an electrothermometer, the detector of which is fixed to the internal surface of the ear. The dilation of the auricular vessels is also examined under the microscope, observations being made on the lumen of the marginal artery and vein[1]. |
References: [1]. Mashkovskii MD, et al. The action of tropaphen on the peripheral vessels. Pharmacology. 1964. 58. 69-71. | |
Tropodifene (Tropaphen) is an α-Adrenergic receptor inhibitor.
Tropaphen has a beneficial effect on hypertension. The therapeutic effect of this preparation is more constant in diseases accompanied by spasm of the peripheral vessels. Tropaphen has a very marked adrenolytic and vasodilator action. It greatly lowers the tone of the peripheral vessels. The preparation is effective starting with a dose of 0.1 mg/kg. After injection of the drug in a dose of 0.25 mg/kg, a considerable and gradually progressive decrease in the perfusion pressure takes place. The pressure falls by 30-35% and remained at a low level for 90-100 min. With a dose of tropaphen of 0.5 mg/kg, the perfusion pressure falls by 40-45% and remains low for 120 min or more. Strong vasodilatation is also observed after injection of tropaphen into intact rabbits[1].
[1]. Mashkovskii MD, et al. The action of tropaphen on the peripheral vessels. Pharmacology. 1964. 58. 69-71.
| Cas No. | 15790-02-0 | SDF | |
| 别名 | 托泊地芬,Tropaphen | ||
| Canonical SMILES | O=C(O[C@H]1C[C@H](N2C)CC[C@H]2C1)C(C3=CC=CC=C3)CC4=CC=C(OC(C)=O)C=C4 | ||
| 分子式 | C25H29NO4 | 分子量 | 407.5 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.454 mL | 12.2699 mL | 24.5399 mL |
| 5 mM | 0.4908 mL | 2.454 mL | 4.908 mL |
| 10 mM | 0.2454 mL | 1.227 mL | 2.454 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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[Effect of the beta-adrenoblocker alpheprol and the alpha-adrenolytic Tropaphen on tolerance to strophanthin in experimental myocardial infarct]
Biull Eksp Biol Med 1980 Oct;90(10):444-6.PMID:6107131doi
The tolerance to strophanthin was studied in acute and subacute experiments on 76 cats at varying time after occlusion of the coronary artery branch. The beta-adrenoblocker alpheprol completely smoothed away the hypersensitivity to strophanthin after the coronary blood flow cessation while the alpha-adrenolytic Tropaphen virtually did not affect the tolerance to strophanthin in intact animals even after experimental myocardial infarction.
[Tropaphen in experimental drug therapy of cor pulmonale]
Biull Eksp Biol Med 1992 Sep;114(9):244-6.PMID:1362091doi
The influence of alpha-adrenoblocking drug Tropaphen on cardio- and haemodynamics under experimental lung-heart failure was studied in dogs. The findings suggest effectiveness of Tropaphen administration in such pathology shown by a decrease of lung hypertension and heart overload, significant increase of the contractile activity and relaxation properties of myocardium of both ventricles and in cardiac pump function optimization.
[Effect of obzidan, Tropaphen, adrenaline and euphylline on histamine bronchospasm in guinea pigs]
Farmakol Toksikol 1984 Nov-Dec;47(6):81-4.PMID:6151520doi
It has been demonstrated in experiments on guinea-pigs that the beta-adrenoblocker propranolol (1-2 mg/kg) substantially raises bronchial sensitivity to histamine (10 mg/kg). The alpha-adrenoblocker Tropaphen (2 mg/kg) potentiates the protective action of adrenaline (5 micrograms/kg) and euphylline (8 mg/kg) in bronchospasm induced by histamine (10 micrograms/kg).
[Effect of tropaphene and fentolamin on the spasmogenic effects of adrenaline, noradrenaline, serotonin and other biologically active substances]
Farmakol Toksikol 1978 Mar-Apr;41(2):142-6.PMID:26588doi
Tests conducted in vitro and in vivo demonstrated that Tropaphen, tropine ether of alpha-phenyl-beta-(p-acetoxyphenyl)-propionic acid, an original alpha-adrenoblocking agent, display a marked antiserotonin activity exceeding that of phentolamine. Moreover, Tropaphen is more active that phenolamine by its inhibiting influence on the spasmogenous effects of histamine, angiotensin, bradykinine and prostaglandin E2. In doses of 0.1 and 0.25 mg/kg both drugs had no effect on changes of the arterial pressure in anesthetized rats, caused by the above mentioned biologically active substances.
[Antihistaminic and antiserotonin properties of new complex tropine esters]
Farmakol Toksikol 1979 Jan-Feb;42(1):3-7.PMID:33829doi
The antihistaminic and antiserotonin properties of 16 new tropine esters, analogues of atropine, tropacin and Tropaphen, were studied. All of them were found to lessen the spasmogenic effects of histamine and serotonin. The intensity of the antihistaminic and antiserotonin action of the drugs varied depending upon the structure of the radical at the alpha-carbon atom in the acidic part of the molecule. Both types of the activity are most marked in the desoxymethyl propyl and butyl analogues of atropine. The absence of the oxymethyl group at alpha-carbon in the series of atropine analogues is shown to facilitate the manifestation of the antihistaminic activity.