83846-83-7
ketanserin tartrate
CAS: 83846-83-7
Molecular Formula: C26H28FN3O9
83846-83-7 - Names and Identifiers
| Name | ketanserin tartrate |
| Synonyms | kjk-945 R 41468 ketanserin tartrate R 41468 TARTRATE SALT KETANSERIN HYDROGEN TARTRATE 4(1h,3h)-quinazolinedione,3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-( 3-(2-(4-(p-fluorobenzoyl)-1-piperidinyl)ethyl)-2,4(1h,3h)-quinazolinedionel 3-[2-[4-(4-fluorobenzoyl)piperidino]ethyl]quinazoline-2,4(1H,3H)-dione [R-(R*,R*)]-tartrate |
| CAS | 83846-83-7 |
| EINECS | 281-062-8 |
| InChI | InChI=1/C22H22FN3O3.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h1-8,16H,9-14H2,(H,24,29);1-2,5-6H,(H,7,8)(H,9,10)/t;1-,2+ |
83846-83-7 - Physico-chemical Properties
| Molecular Formula | C26H28FN3O9 |
| Molar Mass | 545.52 |
| Melting Point | 183～186℃ |
| Solubility | ethanol: 3.3mg/mL |
| Appearance | solid |
| Color | white |
| Storage Condition | 2-8°C |
| MDL | MFCD00084651 |
| Physical and Chemical Properties | White or off-white powder |
| Use | Selective 5-HT2 5-hydroxytryptamine (serotonin) receptor antagonist. |
| In vitro study | Ketanserin at 0.3 μM inhibits the voltage-dependent step current (I hERG.step ) and tail current (I hERG.tail ) of hERG channels with a 5-min exposure. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC 50 =22.0±7 μM), Ketanserin (IC 50 =152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC 50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM. Ketanserin inhibits platelet aggregation with an IC 50 of 240 (169-339) nM. |
| In vivo study | Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT 2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions. |
83846-83-7 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | VA1411195 |
| HS Code | 29335990 |
| Hazard Class | 6.1 |
| Toxicity | LD50 oral in rat: 129mg/kg |
83846-83-7 - Reference Information
| specification | ketostilbene tartrate tablets: 20mg/tablet, 40mg/tablet. Injection: 5mg/1ml,10mg/2ml,25mg/5ml. |
| dosage | ketostilbene tartrate oral, 20mg, bid. After 1 month, if the effect is not satisfactory, it can be increased to 40mg/Times, 2 times a day, when the dose exceeds 40mg, the antihypertensive effect is no longer enhanced. Hepatic insufficiency, each dose should not exceed 20mg. The intravenous dose is 10mg, the maximum dose is 30mg, injected at a rate of 3mg per minute. Can also be intravenous drip, drip Speed 2-6mg/h |
| adverse reactions | dizziness, fatigue, edema, dry mouth, weight gain and Q-Tc prolongation (prone to hypokalemia). |
| pharmacological action | 1. Ketosserin tartrate in the treatment of pregnancy-induced hypertension syndrome and pre-eclampsia Although ketosserin is an anti-hypertensive drug available, but the clinical reports of its treatment of essential hypertension are few, there are many reports on the clinical observation of the prevention and treatment of the pregnancy induced hypertension syndrome, preeclampsia and HELLP syndrome. Most reports suggest that ketanserin has certain preventive and therapeutic effects on pregnancy-induced hypertension, preeclampsia and HELLP syndrome. The ketoserin group significantly reduced diastolic blood pressure, while systolic blood pressure also decreased but had no significant effect, and this difference could be monitored from the 7th day of administration. The curative effect of ketanserin on preeclampsia is better than that of hydrochlorothiazide. In addition, 2 cases were observed in clinical cases, all of which were elderly pregnant women, who did not use ketanserin in their first pregnancy. All of them had high risk factors such as hemolysis, thrombocytopenia and eclampsia, she received oral ketoresin and aspirin anticoagulants during her second pregnancy. The self-control of these 2 high-risk pregnant women also suggested that ketostilin had a preventive effect on pregnancy-induced hypertension and preeclampsia. In the prevention and treatment of pregnancy-induced hypertension, whether ketanserin has adverse effects on fetal development is also concerned. Some studies have shown that the placental barrier pass rate of ketoxylin is high; After delivery, ketoxylin and its metabolites are eliminated within 13.8~34.4H in the newborn. 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. Therefore, the clinical observation of 44 patients with stable angina pectoris caused by single vessel blockage showed that, intracoronary injection of ketoresen (1.5mg in 10ml of 0.9% sodium chloride solution, 3min after injection) during coronary balloon angioplasty can significantly increase coronary collateral blood flow to reduce the occurrence of myocardial ischemia. The authors believe that the results of this experiment not only indicate that ketostilbene has the effect of preventing myocardial ischemia in coronary artery balloon angioplasty, it is also suggested that ketanserin may have a new application in the treatment of myocardial ischemia. |
| biological activity | Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also inhibited the hERG current (IhERG) with an IC50 of 0.11 μm in a concentration-dependent manner. |
Last Update：2024-04-09 21:01:54
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