Aligeron
目录号 : GC32558
Aligeron是一种非选择性的prostaglandin(PG)拮抗剂，具有舒张血管的作用。
Cas No.:70713-45-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.
Aligeron shows a broad spectrum of antagonistic action against different spasmogens in different isolated organs. The experiments on isolated perfused rabbit artery shows the antagonistic action of aligeron against the vasoconstrictor effects of noradrenaline and adrenaline[1]. The effect of aligeron in vitro lacks selectivity and is probably due to interference with the action of Ca2+[3].
In hypoventilation hypoxia, aligeron (5 mg/kg i.v.) and cinnarizine increase cortical resistance to hypoxia and accelerated the recovery of cortical bioelectrical activity. In KCl- and AMP-induced depressions aligeron shows a protective effect manifested in a decrease of the degree and duration of the depression[2].
[1]. Miyares K, et al. Antagonistic activity of aligeron and papaverine against different smooth muscle stimuli. Methods Find Exp Clin Pharmacol. 1985 Sep;7(9):473-6. [2]. Dimov S, et al. Effect of aligeron and cinnarizine in models of general and local depression of the cortical bioelectrical activity in cats. Methods Find Exp Clin Pharmacol. 1983;5(2):89-95. [3]. Nikolov R, et al. Study on the prostaglandin antagonistic activity of aligeron and piracetam. Methods Find Exp Clin Pharmacol. 1982 Aug-Sep;4(6):387-95.
| Cas No. | 70713-45-0 | SDF | |
| Canonical SMILES | C=CCN1CCN(C(C2=CC=CC=C2)C3=CC=CC=C3)CC1 | ||
| 分子式 | C20H24N2 | 分子量 | 292.42 |
| 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 | 3.4197 mL | 17.0987 mL | 34.1974 mL |
| 5 mM | 0.6839 mL | 3.4197 mL | 6.8395 mL |
| 10 mM | 0.342 mL | 1.7099 mL | 3.4197 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 | ||||||||||
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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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effect of Aligeron on the cerebral venous outflow and cerebrospinal fluid pressure in dogs
Methods Find Exp Clin Pharmacol 1981 Jul-Aug;3(4):213-6.PMID:7278433doi
The effect of Aligeron (1-benzhydril-4-allyl-piperazine dihydrochloride) on the cranial circulation was studied in dogs under chloralose-urethan anaesthesia. The parameters followed were: venous outflow from the confluence of the cerebral sinusses (CVO), cerebrospinal fluid pressure in cysterna magna (CSFP), systemic arterial blood pressure (BP) and pulse rate (PR). CVP was measured using the technique of Rapela and Green (1964). Aligeron was applied at doses of 5 and 10 mg/kg i.v. Papaverine hydrochloride was used as a reference compound. Aligeron administration at a dose of 5 mg/kg led to quick increase of the CVO with a duration of the effect approximately 30 min. CSFP also increased in a similar way. BP and PR showed insignificant changes. The administration of 10 mg/kg did not lead to an increase of its effect on CVO. Papaverine (1 mg/kg i.v.) had a weaker effect than that of Aligeron. According to the classical concepts the changes observed in our experiments were due to the cerebral vasodilator effect of Aligeron which caused a fall in cerebrovascular resistance and an increase of the intracranial blood volume. Our experiments suggest that Aligeron influenced the resistance vessels more than the capacitance ones.
Effect of Aligeron on the resistance of the cerebral and peripheral blood vessels
Acta Physiol Pharmacol Bulg 1980;6(3):54-9.PMID:7282382doi
The effect of the cinnarizine analogue Aligeron on the resistance of cerebral and peripheral blood vessels was studied in acute experiments on cats and dogs. The resistance of the cerebral vessels was determined directly and indirectly. For direct determination the method of autoperfusion was used. The resistance was calculated indirectly as a quotient of mean arterial blood pressure and internal carotid blood flow. For evaluation of Aligeron effect on the resistance of the peripheral blood vessels and method of autoperfusion of the femoral artery was used. Aligeron was administered i. v. and i. a. In some of the experiments the compound was applied on the background of previously injected dihydroergotamine. Cinnarizine and papaverine were used as reference compounds. The results show that Aligeron decreases considerably the cerebral and peripheral resistance vessels tone, and its effect is higher than those of cinnarizine. For the realization of this effect most probably its direct myotropic action plays the main role. The reduction of its effect after alpha-adrenergic blockade suggests an involvement of some adrenergic blocking properties in its mechanism of vascular action.
Study on the prostaglandin antagonistic activity of Aligeron and piracetam
Methods Find Exp Clin Pharmacol 1982 Aug-Sep;4(6):387-95.PMID:6958951doi
The interaction of Aligeron and piracetam with the effects of prostaglandin F2 alpha (PGF2 alpha) E2 (PGE2) was studied using in vitro and in vivo tests for evaluation of PG antagonistic activity. Aligeron was found to be a non-selective PG antagonist in isolated guinea-pig stomach smooth muscle preparations. It antagonized the PGF2 alpha and PGE2-induced fall in blood pressure in cats prevented diarrhoea induced by PGF2 alpha in mice, inhibited rat paw oedema induced by PGE2 in rats, but did not modify the PGF2 alpha induced bronchoconstriction in guinea-pigs. Piracetam did not antagonize the smooth muscle contractile effects of PGF2 alpha and PGE2 and in the in vivo tests it inhibited only the rat paw oedema induced by PGE2. It is concluded that Aligeron is active in vitro and in vivo as an antagonist of some of the actions of PGs studied. Its effect in vitro lacks selectivity and is probably due to interference with the action of Ca2+. The probable clinical implication of these results will be discussed. Piracetam can not be considered a PG antagonist.
Effect of Aligeron and cinnarizine in models of general and local depression of the cortical bioelectrical activity in cats
Methods Find Exp Clin Pharmacol 1983;5(2):89-95.PMID:6308367doi
The effect of Aligeron (5 mg/kg i.v.) and cinnarizine (10 mg/kg i.v.) on general and local depression of cortical bioelectrical activity was studied in acute experiments on cats. Asphyxic anoxia and hypoventilation hypoxia were used as models of general depression. Local depressions were caused by topical application of potassium chloride (KCl) and adenosine-5'-monophosphate (AMP) on the cortex. In hypoventilation hypoxia Aligeron and cinnarizine increased cortical resistance to hypoxia and accelerated the recovery of cortical bioelectrical activity. In KCl- and AMP-induced depressions the drugs showed a protective effect manifested in a decrease of the degree and duration of the depression. In asphyxic anoxia their effect was insignificant.
Antagonistic activity of Aligeron and papaverine against different smooth muscle stimuli
Methods Find Exp Clin Pharmacol 1985 Sep;7(9):473-6.PMID:4079597doi
The antagonistic action of Aligeron as compared to that of papaverine against different smooth muscle stimuli was studied in experiments in vitro. Three series of experiments were conducted: study of the antagonistic action against experimental spasms of isolated organs caused by different spasmogens; determination of the type of antagonism to adrenaline in isolated vas deferens preparation; and study of the antagonistic action against vasoconstrictor effects of noradrenaline and adrenaline in isolated perfused rabbit renal artery. Aligeron showed a broad spectrum of antagonistic action against different spasmogens in different isolated organs. Its effect was more pronounced than that of papaverine. The antagonism was of the non-competitive type. The experiments on isolated perfused rabbit artery showed the antagonistic action of Aligeron against the vasoconstrictor effects of noradrenaline and adrenaline. The results suggest the clinical use of Aligeron in conditions associated with increased release of these vasoactive substances.