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CAS No.: 74050-98-9

Ketanserin/凯他色林 Catalog No. CSN16459

Synonyms: R41468;酮色林

Ketanserin is a specific 5-HT2A serotonin receptor antagonist with K_i of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Ketanserin is a serotonin S2-receptor antagonist introduced for the treatment of arterial hypertension and vasospastic disorders. Following oral administration ketanserin is almost completely (more than 98%) and rapidly absorbed and peak concentrations in plasma are reached within 0.5 to 2 hours. Following intravenous administration plasma ketanserin concentrations decay triexponentially with sequential half-lives of 0.13, 2 and 14.3 h^[3]. Ketanserin, a selective 5-HT receptor antagonist, prolongs the QT interval of ECG in patients. Ketanserin blocked hERG current (I(hERG)) in a concentration-dependent manner (IC50=0.11 mM). The drug showed an open channel blocking property, the block increasing significantly at depolarizing voltages between +10 to +60 mV. Voltage-dependence for inactivation of hERG channels was negatively shifted by 0.3 mM ketanserin. A 2.8 fold attenuation of inhibition by elevation of external K+ concentration (from 5.0 to 20 mM) was observed, whereas the inactivation-deficient mutants S620T and S631A had the IC50s of 0.84 +/- 0.2 and 1.7 +/-0.4 mM (7.6 and 15.4 fold attenuation of block)^[4]. It also inhibits the effects of serotonin on platelets in cardiovascular disease, inhibits vasoconstriction caused by the amine, and when administered intravenously improves some haemorheological indices in patients with ischaemic diseases. Administered intravenously, ketanserin 10mg followed by an infusion of 2 to 4 mg/h controls moderate to severe pre- and postoperative hypertension in most patients, acting as a balanced vasodilator, lowering cardiac pre- and afterload{{Brogden RN, Sorkin EM. Ketanserin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in hypertension and peripheral vascular disease. Drugs. 1990;40(6):903‐949|https:// www.ncbi. nlm.nih.gov/ pubmed/2079001}}.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03321136	Healthy	Early Phase 1	Recruiting	March 2019	Switzerland ... more >> University Hospital Recruiting Basel, Switzerland, 4031 Contact: Matthias E Liechti, Prof. Dr. med. matthias.liechti@usb.ch Contact: Friederike Holze, MSc friederike.holze@usb.ch Collapse <<
NCT01778686	Healthy	Not Applicable	Completed	-	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Copenhagen, Denmark, 2100 Collapse <<
NCT03289949	Basic Science	Phase 1	Recruiting	December 31, 2019	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Recruiting Copenhagen, Denmark, 2100 Contact: Gitte M Knudsen, Professor Collapse <<

更多
参考文献

[1] Lakoski JM, Aghajanian GK. Effects of ketanserin on neuronal responses to serotonin in the prefrontal cortex, lateral geniculate and dorsal raphe nucleus. Neuropharmacology. 1985 Apr;24(4):265-73.
[2] Van Nueten JM, Janssen PA, et al. Vascular effects of ketanserin (R 41 468), a novel antagonist of 5-HT2 serotonergic receptors. J Pharmacol Exp Ther. 1981 Jul;218(1):217-30.
[3] Persson B, Heykants J, Hedner T. Clinical pharmacokinetics of ketanserin. Clin Pharmacokinet. 1991;20(4):263‐279
[4] Tang Q, Li ZQ, Li W, et al. The 5-HT2 antagonist ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels. Br J Pharmacol. 2008;155(3):365‐373

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5289 mL
- 12.6445 mL
- 25.2889 mL
- 5 mM
- 0.5058 mL
- 2.5289 mL
- 5.0578 mL
- 10 mM
- 0.2529 mL
- 1.2644 mL
- 2.5289 mL

技术信息

CAS号

74050-98-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H22FN3O3

运输

蓝冰

分子量

395.43

别名

R41468;酮色林

溶解度

DMSO	2 mg/ml (5.06 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

4% DMSO+40% PEG 300+4% Tween 80+water

1 mg/mL

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03321136	Healthy	Early Phase 1	Recruiting	March 2019	Switzerland ... more >> University Hospital Recruiting Basel, Switzerland, 4031 Contact: Matthias E Liechti, Prof. Dr. med. matthias.liechti@usb.ch Contact: Friederike Holze, MSc friederike.holze@usb.ch Collapse <<
NCT01778686	Healthy	Not Applicable	Completed	-	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Copenhagen, Denmark, 2100 Collapse <<
NCT03289949	Basic Science	Phase 1	Recruiting	December 31, 2019	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Recruiting Copenhagen, Denmark, 2100 Contact: Gitte M Knudsen, Professor Collapse <<
NCT01329887	Severe Sepsis ... more >> Septic Shock Collapse <<	Phase 3	Completed	-	Netherlands ... more >> Medical Centre Leeuwarden Leeuwarden, Netherlands Collapse <<
NCT02451072	Healthy	Not Applicable	Completed	-	Switzerland ... more >> Center for Psychiatric Research, Department of Psychiatry, Psychotherapy and Psychosomatic, Psychiatric Hospital, University of Zurich Zurich, Switzerland, 8032 Collapse <<
NCT00557219	Acute Renal Failure	Phase 3	Terminated(Main cooperator fin... more >>ished cooperation) Collapse <<	-	Poland ... more >> Department of Cardiac Anesthesiology, Medical University of Gdańsk Gdańsk, Poland, 80-211 Collapse <<
NCT02632877	Diabetic Foot Ulcer	Phase 1 Phase 2	Completed	-	Mexico ... more >> Molecular Biology and Gene Therapy Institute Guadalajara, Jalisco, Mexico, 44340 Hospital Valentín Gómez Farías Zapopan, Jalisco, Mexico Collapse <<
NCT03646318	Critical Illness	Phase 4	Not yet recruiting	May 1, 2019	-

Ketanserin/凯他色林 Catalog No. CSN16459

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