Ketanserine [INN-French]
ketanserin
CAS: 74050-98-9
Molecular Formula: C22H22FN3O3
Ketanserine [INN-French] - Names and Identifiers
| Name | ketanserin |
| Synonyms | p73H OFC8 EEC3 p53CP B(p51A) B(p51B) R 41,468 Ketaserin ketanserin Ketanserine Ketanserina Ketanserinum UNII-97F9DE4CT4 p63, GST tagged human Ketanserine [INN-French] Ketanserinum [INN-Latin] Ketanserina [INN-Spanish] 3-(2-(4-(p-Fluorobenzoyl)piperidino)ethyl)-2,4-(1H,3H)-quinazolinedione 3-{2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl}quinazoline-2,4(1H,3H)-dione 2,4(1H,3H)-Quinazolinedione, 3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)- |
| CAS | 74050-98-9 |
| EINECS | 277-680-2 |
| InChI | InChI=1/C22H22FN3O3/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29) |
Ketanserine [INN-French] - Physico-chemical Properties
| Molecular Formula | C22H22FN3O3 |
| Molar Mass | 395.43 |
| Density | 1.280±0.06 g/cm3(Predicted) |
| Melting Point | 227-235°C |
| Solubility | Soluble in water (<1 mg/ml at 25 °C), DMSO (2 mg/ml at 25 °C), ethanol (<1 mg/ml |
| Appearance | Solid |
| Color | White to Off-White |
| Merck | 14,5296 |
| pKa | 7.5(at 25℃) |
| Storage Condition | Sealed in dry,2-8°C |
| Refractive Index | 1.592 |
| Physical and Chemical Properties | Crystallization from 4-methyl-2-pentanone, melting point 227-235 °c. Solubility (g/100ml): Water 0.001, ethanol 0.038, dimethylformamide 2.34. pKa 7.5. |
| Use | For the treatment of hypertension medication |
Ketanserine [INN-French] - Risk and Safety
| WGK Germany | 3 |
| RTECS | VA1411190 |
| HS Code | 29339900 |
Ketanserine [INN-French] - Introduction
Ketanserin is a specific 5-HT2A 5-hydroxytryptamine receptor antagonist, acting on rat and human 5-HT2A,Ki is 2.5 nM.
Last Update：2022-10-16 17:28:15
Ketanserine [INN-French] - Reference Information
| Clinical application | 1. Treatment of pregnancy-induced hypertension syndrome and Preeclampsia: Although ketanserin is an antihypertensive drug, however, there are few clinical reports on the treatment of essential hypertension, and the use of ketostilbene in pregnancy-induced hypertension syndrome, preeclampsia and HELLP syndrome (hemolysis, elevated liver enzymes and thrombocytopenia syndrome) the prevention and treatment of clinical observation reported more. Most reports suggest that ketanserin has certain preventive and therapeutic effects on pregnancy-induced hypertension, preeclampsia and HELLP syndrome. According to the majority of clinical observations, ketanserin for the majority of pregnancy-induced hypertension syndrome, preeclampsia and other pregnancy-induced hypertension complications have a better therapeutic effect, and has not yet found its significant adverse effects on the fetus. As for some patients with ketoxylin efficacy is not ideal, should be further beyond the pharmacokinetic reasons. 2. Application of coronary artery balloon angioplasty coronary artery balloon angioplasty is a common surgical method for the treatment of myocardial ischemia caused by tubular artery stenosis. But in the coronary artery balloon angioplasty because of the stenosis of the coronary artery into the coronary stent, sometimes immediately the original stenosis of the distal coronary artery contraction, causing myocardial ischemia, it is speculated that this coronary artery constriction may be caused by 5-HT. The experimental results not only indicate that ketanserin has the effect of preventing myocardial ischemia in coronary artery balloon angioplasty, but also suggest that ketanserin may have a new application in the treatment of myocardial ischemia. |
| Use | 1. Treatment of Cushing's syndrome: because the formation of thalamic-pituitary Cushing's syndrome is associated with central 5-HT neurons. Thus, attempts have been made to treat pituitary Cushing's syndrome with ketanserin. Subjects were given ketanserin 40-80 mg/d, and urinary cortisol and adrenocorticotropic hormone (ACTH) were monitored. Therefore, it is considered that the treatment of Cushing's syndrome with ketoranserin may have a certain effect, but the duration of its efficacy and the number of patients with marked effect are limited. But after all, this experiment provides a new idea for the pathogenesis and treatment of thalamic-pituitary Cushing's syndrome. 2. Treatment of leg and foot ulcers in diabetic patients: diabetic leg and foot ulcers are a complication of diabetes that is difficult to treat, the patient was at risk for amputation. Topical application of 2% ketosolin ointment has been tried to treat diabetic leg and foot ulcers. Its therapeutic mechanism may be related to blocking α receptor and dilating blood vessels to improve local circulation. The results of this study not only provide a new therapeutic approach for the treatment of leg and foot ulcers in diabetic patients, but also expand the range of clinical applications of ketanserin. selective antagonists of serotonin s2-receptors, without agonistic activity, with weak αl-and H1-antagonistic activity, but without effect on other receptors. For the control of mild, moderate or severe hypertension, can also be used to control acute hypertension attack, such as before or after surgery and maternal preeclampsia. medication for hypertension |
| production method | Method 1: condensation of compound (I) with 4-(4-fluorobenzoyl) piperidine, ketanserin was obtained. Method 2: compound (II) and 4-(4-fluorobenzoyl) piperidine, sodium carbonate were heated in 5-methyl -2-pentanone to give ketorin. |
Last Update：2024-04-10 22:29:15
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