PIRIBEDIOL
piribedil
CAS: 3605-01-4
Molecular Formula: C16H18N4O2
PIRIBEDIOL - Names and Identifiers
| Name | piribedil |
| Synonyms | ET-495 EU-4200 piribedil PIRIBEDIL Piribendyl PIRIBEDIOL 1-(2-Pyrimidyl)-4-piperonylpiperazine 2[4-(1,3-benzodioxol-5-ylmethyl)-1-piperazinyl-]pyrimidine 2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]pyrimidine 2-(4-(benzo[d][1,3]dioxol-5-ylMethyl)piperazin-1-yl)pyriMidine |
| CAS | 3605-01-4 |
| EINECS | 222-764-6 |
| InChI | InChI=1/C16H18N4O2.CH4O3S/c1-4-17-16(18-5-1)20-8-6-19(7-9-20)11-13-2-3-14-15(10-13)22-12-21-14;1-5(2,3)4/h1-5,10H,6-9,11-12H2;1H3,(H,2,3,4) |
PIRIBEDIOL - Physico-chemical Properties
| Molecular Formula | C16H18N4O2 |
| Molar Mass | 298.34 |
| Density | 1.1183 (rough estimate) |
| Melting Point | 98° |
| Boling Point | 439.76°C (rough estimate) |
| Flash Point | 237.7°C |
| Solubility | Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly) |
| Vapor Presure | 5.54E-09mmHg at 25°C |
| Appearance | Solid |
| Color | White |
| Merck | 14,7493 |
| pKa | 7.17±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.6000 (estimate) |
PIRIBEDIOL - Risk and Safety
| RTECS | UV9704000 |
| Toxicity | LD50 in mice (mg/kg): 88 i.v., 690 i.p., 1460 orally (Laubie) |
PIRIBEDIOL - Reference Information
| Vasodilators | Piribedil, also known as teasudar, piperidone, and dipiperazine, is a commonly used clinical peripheral blood vessels And cerebrovascular dilators are dopamine receptor agonists. They can be used alone or in combination with levodopa to treat Parkinson's disease and improve certain symptoms caused by mental defects in the elderly, adjuvant treatment of intermittent claudication (stage 2) caused by decreased attention and memory, vertigo, and arterial embolism of the lower extremities. Retinal defect attacks improve visual acuity, the effect is similar to dopamine, and the side effects are similar to levodopa. In addition, this product can also improve peripheral blood circulation, and has a certain effect on obstructive or embolic fundus diseases. pirbedil can stimulate D2 receptors after nigrostriatal synapses and D2 and D3 receptors in midbrain cortex and midbrain marginal lobe pathways, providing effective dopamine effect. During the treatment, pirbedil occurs in the "dopaminergic" type to stimulate the electrogenesis of the cerebral cortex, which has clinical effects on various functions caused by dopamine. For peripheral circulation, this drug can increase femoral blood flow. This mechanism of action may be due to inhibition of sympathetic nerve tone. Oral absorption is rapid, Tmax is 1h. The plasma protein binding rate is low. Therefore, there is little possibility of interaction between this drug and other drugs. T1/2 is 1.7~6.9h. The drug has two metabolites, one is a monohydroxy derivative and the other is a dihydroxy derivative. The absorbed pirbedor 68% is excreted from the kidney in the form of metabolites, and is completely removed at about 50% and 48h in 24h, with 25% excreted from bile. The drug can gradually release the active ingredients, and the therapeutic effect can last for more than 24 hours. |
| indications | for tremor syndrome. Can be used as a single drug. Special treatment of patients with tremor as the main symptom. It can also be used in combination with levodopa as an initial or later treatment. Used for pain. It can relieve spasmolysis and pain. It can be used for painful symptoms (such as painful spasm while walking). used for peripheral circulation disorders. Take its effect of activating blood and dredging collaterals to treat the circulating blood volume and blood flow per minute caused by the obstruction of meridians and blood stasis, blood concentration, and then systemic hypoxia, and the central regulation of cerebral circulation. |
| usage and dosage | treatment of tremor syndrome: the dose is gradually increased, and the maintenance dose for treatment alone is 150~250mg per day, which is taken after 3 meals. When pirbedil is combined with levodopa, the general maintenance dose is 50~150mg per day. Other indications: 50mg daily, taken after main meal. In severe cases, 100mg daily, divided into 2 doses. Parkinson's disease: take this product orally, 3 times a day, 50mg each time, after meals; if levodopa is used, the product can be appropriately reduced, and the daily dose is controlled at 50~100mg, can be taken 1~3 times. Peripheral circulation disorder: once a day, 50mg is enough. In severe cases, 100mg can be taken twice. |
| adverse reactions and precautions | mild gastrointestinal reactions, such as nausea, vomiting and flatulence, can be treated with domperidone. Take the medicine or adjust the dose between meals, and add the antagonist of CTZ (domperidone) can reduce the occurrence of side effects. Abnormal blood pressure (orthostatic hypotension) or drowsiness is rare. If the therapeutic dose for Parkinson's disease patients needs to be increased, it should be completed gradually. Generally, the daily dose should not exceed 250mg. This product is a sustained-release preparation, do not bite when taking it, but swallow it whole. Patients with circulatory failure and acute myocardial infarction are contraindicated. piribedil is not a substitute for specific antihypertensive therapy in hypertensive patients. There is still a lack of information on this aspect for pregnant and lactating women, and this risk is not completely clear. |
| Biological activity | Piribedil is a dopamine D2 receptor (D2R) agonist, which also shows antagonism to hα1A-adrenoceptor (hα1A-AR). |
| Target | Value |
| D3 receptor () | |
| adrenoceptor α2C (CHO) | 7.2(pKi) |
| adrenoceptor α2A (CHO) | 7.1(pKi) |
| D2 receptor (CHO) | 6.9(pKi) |
Last Update：2024-04-10 22:29:15
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Product Name: piribedil；2-[4-(1,3-Benzodioxol-5-ylmethyl)piperazin-1-yl]pyrimidine Request for quotationCAS: 3605-01-4
Tel: +86 19849939632
Email: 2470479589@qq.com
Mobile: +86 19849939632
QQ: 2470479589
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Spot supply
Product Name: Piribedil Visit Supplier Webpage Request for quotationCAS: 3605-01-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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