Tolonidine
(Synonyms: 托洛尼定) 目录号 : GC38866
Tolonidine 是咪唑啉的衍生物。Tolonidine 是口服有效的，且具有降高血压和抗高血压作用。
Cas No.:4201-22-3
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
Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties[1].
In the anesthetized dog, tolonidine administered i.v. decreases the amplitude of ventricular contractions, reduces aortic blood flow and increases peripheral vascular resistances[1]. In the bivagotomized pithed rat, tolonidine induces a long-lasting increase in blood pressure with no secondary hypotension, thus suggesting peripheral sympathomimetic properties[1].
[1]. Cosnier D, et al. Pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (tolonidine), a new antihypertensive agent. II. Action on cardiac contraction, circulatory parameters, autonomic receptors and diuresis. Arzneimittelforschung. 1975 Nov;25(11):1802-6.
| Cas No. | 4201-22-3 | SDF | |
| 别名 | 托洛尼定 | ||
| Canonical SMILES | CC1=CC=C(NC2=NCCN2)C(Cl)=C1 | ||
| 分子式 | C10H12ClN3 | 分子量 | 209.68 |
| 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 | 4.7692 mL | 23.8459 mL | 47.6917 mL |
| 5 mM | 0.9538 mL | 4.7692 mL | 9.5383 mL |
| 10 mM | 0.4769 mL | 2.3846 mL | 4.7692 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (Tolonidine), a new antihypertensive agent. I. Action on blood pressure and heart rate
Arzneimittelforschung 1975 Oct;25(10):1557-61.PMID:1243037doi
Tolonidine, 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate, a substance structurally related to clonidine, was studied for its effects on blood pressure and heart rate in anesthetized or conscious, normotensive or hypertensive animals (mainly dogs). In all cases, blood pressure was lowered by Tolonidine. Initial short-lasting hypertension was observed after each i.v. administration. Heart rate was markedly lowered irrespective of the experimental process. Comparison with clonidine, guanethidine and mecamylamine in hypertensive anesthetized or unanesthetized animals made it possible to place Tolonidine with respect to these reference antihypertensive drugs. A close relationship essentially appears between the effects of both derivatives of imidazoline: Tolonidine and clonidine, Tolonidine being, however, active at higher doses. The analysis of these results will appear at the end of a series of three articles.
Pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (Tolonidine), a new antihypertensive agent. III. Action on the secretions of the digestive tract and on the central nervous system, acute toxicity
Arzneimittelforschung 1975;25(12):1926-33.PMID:3186doi
The pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (Tolonidine) a new synthetic derivative of imidazoline are reported in a series of three successive articles. This compound has been shown to possess hypotensive and antihypertensive properties. After i.v. administration, the hypotensive phase was preceded by hypertension related to the potent direct alpha-sympatheticomimetic properties of the product. This pressor response, which was not seen after oral administration, was accompanied by a marked decrease in cardiac output and a significant increase in peripheral vascular resistance. The hypotensive action of the product was due to a drop in cardiac output probably reinforced by a decrease in vasoconstrictor sympathetic tone due to a central action. Whatever the route of administration, Tolonidine slowed heart rate independently of blood pressure variations, due essentially to an increase in vagal tone. In studies of diuresis, liquid and salt loss were observed in the cat, not in the dog. At doses which induce a drop in blood pressure Tolonidine did not produce a reduction in pilocarpine-induced salivary secretion and only partially inhibited gastric secretion. In the central nervous system, Tolonidine produced a sedation which first appeared at doses having an antihypertensive effect but which was only fully apparent with increased doses. A decrease in the release of cerebral amines, serotonin and noradrenaline by Tolonidine is proposed. Tolonidine was compared with three other antihypertensive agents: clonidine, which is structurally related, and guanethidine and mecamylamine, which are structurally unrelated and have a different mode of action. A close resemblance of the pharmacological properties of Tolonidine and clonidine was established due to the chemical relationship between the two substances.
Behavioral and electrocortical effects of Tolonidine in rats
Res Commun Chem Pathol Pharmacol 1986 Dec;54(3):299-312.PMID:3797809doi
The rats systemic administration of Tolonidine in rats (0.05-5.0 mumol/Kg) produced behavioural and electrocortical slow-wave sleep lasting between 35 and 200 min depending on the dose. In addition, a dose-dependent fall in deep body temperature was observed. Similar effects were evoked by infusing Tolonidine (5-80 nmol) into the third cerebral ventricle. Behavioural, ECoG and body temperature effects were prevented by previous intraventricular or systemic injection of phentolamine, an antagonist at alpha 1- and alpha 2-adrenoceptors, and of yohimbine, an antagonist at alpha 2-adrenoceptors, whereas prazosin, an alpha 1-adrenoceptor antagonist, was ineffective. In conclusion, the present experiments show that Tolonidine possesses central effects similar to those evoked by clonidine and provide further evidence in favour of the idea that central alpha 2-adrenoceptors are involved in the control of slow-wave sleep and body temperature.
Pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (Tolonidine), a new antihypertensive agent. II. Action on cardiac contraction, circulatory parameters, autonomic receptors and diuresis
Arzneimittelforschung 1975 Nov;25(11):1802-6.PMID:1243090doi
Tolonidine, 2(2-chloro-p-toluidino)-2-imidazoline-nitrate, is a substance chemically related to clonidine. In the anesthetized dog, Tolonidine administered i.v. decreased the amplitude of ventricular contractions, reduced aortic blood flow and increased peripheral vascular resistances. In the bivagotomized pithed rat, Tolonidine induced a long-lasting increase in blood pressure with no secondary hypotension, thus suggesting peripheral sympathomimetic properties, however, contractions of seminal vesicles in vitro were not obtained. The product proved to have no peripheral sympatholytic or parasympatholytic properties. In the dog and the rat, diuresis was hardly changed. These properties are closely related to those of clonidine, which was studied comparatively. A general discussion is proposed at the end of a third article.