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Catalog No.S2232 Synonyms: R41468

4 publications

Ketanserin  Chemical Structure

CAS No. 74050-98-9

Ketanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.

Selleck's Ketanserin has been cited by 4 publications

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  • Immunofluorescence labeling revealed the comparative protein expression level of c-Myc in the mouse (C57BL/6) hippocampus compared with the control group. ***p < 0.001 vs. sham group, ###p < 0.001 vs. CF+SPS+DMSO group, sssp < 0.001 vs. CF+SPS+ ketanserin group. Bar = 100 μm. Data were presented as mean ± SEM through ANOVA. Groups were compared by performing Bonferroni's test. n = 4.

    Neurosignals, 2017, 25(1):39-53. Ketanserin purchased from Selleck.

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Biological Activity

Description Ketanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.
5-HT2A [7] 5-HT2C (Rat) [7] 5-HT2C (Human) [7]
2.5 nM(Ki) 50 nM(Ki) 100 nM(Ki)
In vitro

Ketanserin causes a dose-dependent inhibition on the contractile responses to 5-hydroxytryptamine of isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, canine gastrosplenic veins and canine saphenous veins. Ketanserin inhibits the contractions of rat caudal arteries and canine saphenous veins caused by postjunctional alpha adrenergic activation. Ketanserin depresses and in certain experiments reverses the vasoconstrictor response to 5-hydroxytryptamine in the perfused guinea-pig stomach. [1] Ketanserin is found to attenuate the excitatory responses produced by norepinephrine, an alpha 1-adrenoceptor-mediated response, in the lateral geniculate nucleus. Ketanserin potentiates rather than attenuates, the inhibitory effect of 5-HT in the lateral geniculate nucleus. [2] Ketanserin significantly prolongs action potential duration (APD) at 50% repolarization by 218% and APD at 90% repolarization by 256% with no significant effect on other action potential parameters in rat ventricular myocytes. Ketanserin results in a concentration- and time-dependent inhibition of charge area of Ito evaluated by integration with an EC50 of 8.3 μM. Ketanserin also blocks Ito and sustained current (ISus) in a dose-dependent manner with an EC50 of 11.2 μM and has no significant effect on both the inward rectifier potassium current and the L-type calcium current. [3]

In vivo Ketanserin produces dose-dependent antinociception in the hot-plate and acetic acid-induced writhing tests with ED50 values (95% confidence limit) of 1.51 and 0.62 mg/kg, respectively, but is without any significant effect on the tail-flick test. [4]


Solubility (25°C)

In vitro DMSO 2 mg/mL (5.05 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+40% PEG 300+4% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 395.43


CAS No. 74050-98-9
Storage powder
in solvent
Synonyms R41468
Smiles C1CN(CCC1C(=O)C2=CC=C(C=C2)F)CCN3C(=O)C4=CC=CC=C4NC3=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03289949 Recruiting Drug: Psilocybine|Drug: Ketanserin Basic Science Gitte Moos Knudsen|Rigshospitalet Denmark March 3 2017 Phase 1
NCT01329887 Completed Drug: ketanserin Severe Sepsis|Septic Shock Medical Centre Leeuwarden March 2011 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID