| Identification | More | [Name]
KETANSERIN TARTRATE | [CAS]
83846-83-7 | [Synonyms]
3-[2-[4-(4-FLUOROBENZOYL)-1-PIPERDINYL]ETHYL]-2,4(1H,3H)-QUINAZOLINEDIONE
3-[2-[4-(4-FLUOROBENZOYL)-1-PIPERDINYL]ETHYL]-2,4(1H,3H)-QUINAZOLINEDIONE TARTRATE
3-[2-[4-(4-FLUOROBENZOYL)-1-PIPERIDINYL]ETHYL]-2,4[1H,3H]-QUINAZOLINEDIONE TARTRATE
3-(2-[4-(4-FLUOROBENZOYL)-1-PIPERIDINYL]ETHYL)-2,4(1H,3H)-QUINAZOLINEDIONE TARTRATE SALT
3-[2-(4-FLUOROBENZOYL)-1-PIPERDINYL]-ETHYL]-2,4(1H,3H)-QUINAZOLINEDIONE TARTRATE
KETANSERIN TARTRATE
KETANSERIN TARTRATE SALT
R 41468
R 41468 TARTRATE SALT
3-(2-(4-(p-fluorobenzoyl)-1-piperidinyl)ethyl)-2,4(1h,3h)-quinazolinedionel
4(1h,3h)-quinazolinedione,3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-(
kjk-945
r-(r*,r*))-2,3-dihydroxybutanedioate(1:1)
3-[2-[4-(4-fluorobenzoyl)piperidino]ethyl]quinazoline-2,4(1H,3H)-dione [R-(R*,R*)]-tartrate
KETANSERIN TARTRATE (R 41468) (SELECTIVE 5-HT2/5-HT1C SEROTONI
Ketanserinetartrate
R 41468 (+)-tartrate salt, 3-(2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl)-2,4(1H,3H)-quinazolinedione (+)-tartrate salt
3-[2-[4-(4-Fluorobenzoyl)piperidino]ethyl]-2,4-(1H,3H)-quinazolinedione tartrate | [EINECS(EC#)]
281-062-8 | [Molecular Formula]
C26H28FN3O9 | [MDL Number]
MFCD00084651 | [Molecular Weight]
545.51 | [MOL File]
83846-83-7.mol |
| Chemical Properties | Back Directory | [Melting point ]
183～186℃ | [storage temp. ]
2-8°C
| [solubility ]
ethanol: 3.3mg/mL
| [form ]
solid
| [color ]
white
| [Water Solubility ]
Soluble to 10 mM in water | [InChIKey]
KMTLTEVOQLMYRS-LREBCSMRSA-N | [SMILES]
O[C@H]([C@@H](O)C(O)=O)C(O)=O.Fc1ccc(cc1)C(=O)C2CCN(CC2)CCN3C(=O)Nc4ccccc4C3=O | [CAS DataBase Reference]
83846-83-7(CAS DataBase Reference) |
| Safety Data | Back Directory | [Hazard Codes ]
T | [Risk Statements ]
R25:Toxic if swallowed. | [Safety Statements ]
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 label where possible) . | [RIDADR ]
UN 2811 6.1/PG 3
| [WGK Germany ]
3
| [RTECS ]
VA1411195
| [HazardClass ]
6.1 | [HS Code ]
29335990 | [Storage Class]
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | [Hazard Classifications]
Acute Tox. 3 Oral | [Toxicity]
LD50 oral in rat: 129mg/kg |
| Hazard Information | Back Directory | [Description]
Ketanserin is a potent antagonist of the serotonin (5-HT) receptor that is selective for 5-HT2 (IC50 = 6.3 nM; Ki = 2.1 nM).1 It has no activity at 5-HT1 receptors but does have activity at histamine type 1, α1-adrenergic, and dopamine receptors with Ki values of 10, 10, and 220 nM, respectively. Ketanserin induces dose-dependent inhibition of contractile responses to 5-HT in isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, and canine gastrosplenic and saphenous veins.2 Ketanserin (10 mg/kg/day) significantly decreases blood pressure (BP), blood pressure variability (BPV), and hypertensive organ damage in spontaneously hypertensive rats.3 Formulations containing ketanserin have been used to treat hypertension in early-onset preeclampsia.4 | [Uses]
coccidiostat | [Uses]
Selective 5-HT2A serotonin receptor antagonist | [Biological Activity]
Selective 5-HT 2A serotonin receptor antagonist; can also be used to discriminate between 5-HT 1D and 5-HT 1B receptor subtypes. | [Biochem/physiol Actions]
Selective 5-HT2 serotonin receptor antagonist. Ketanserin significantly reduces nicotine self-administration in rats, supporting an unexpected involvement of serotonin in nicotine addiction. | [storage]
Room temperature | [References]
[1] J.E. LEYSEN. Receptor binding profile of R 41 468, A novel antagonist at 5-HT2 receptors[J]. Life sciences, 1981, 28 9: Pages 1015-1022. DOI: 10.1016/0024-3205(81)90747-5
[2] J M VAN NUETEN. Vascular effects of ketanserin (R 41 468), a novel antagonist of 5-HT2 serotonergic receptors.[J]. Journal of Pharmacology and Experimental Therapeutics, 1981, 218 1: 217-230.
[3] WEN-MIN DU. Effects of long-term treatment with ketanserin on blood pressure variability and end-organ damage in spontaneously hypertensive rats.[J]. Journal of Cardiovascular Pharmacology, 2003, 41 2: 233-239. DOI: 10.1097/00005344-200302000-00012
[4] SEBASTIAAN W. NIJ BIJVANK . Ketanserin versus dihydralazine for the treatment of severe hypertension in early-onset preeclampsia: a double blind randomized controlled trial[J]. European journal of obstetrics, gynecology, and reproductive biology, 2015, 189: Pages 106-111. DOI: 10.1016/j.ejogrb.2015.02.002 |
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