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Ketanserin

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Chemical Structure| 74050-98-9 同义名 : 酮色林 ;R41468;Ketanserinum
CAS号 : 74050-98-9
货号 : A209484
分子式 : C22H22FN3O3
纯度 : 99%+
分子量 : 395.427
MDL号 : MFCD00083392
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(40.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 5 mg/mL(12.64 mM)，配合低频超声助溶
动物实验配方：

4% DMSO+40% PEG 300+4% Tween 80+water 1 mg/mL

生物活性
靶点

  • 5-HT2

    5-HT2C (Human), Ki:2.5 nM

    5-HT2C (Rat), Ki:50 nM
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}}.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL
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