Ketanserin

Catalog No.S2232 Synonyms: R41468

Ketanserin  Chemical Structure

Molecular Weight(MW): 395.43

Ketanserin 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.

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Biological Activity

Description Ketanserin 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.
Targets
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]

Protocol

Solubility (25°C)

In vitro DMSO 2 mg/mL (5.05 mM)
Water Insoluble
Ethanol Insoluble

* 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
Formula

C22H22FN3O3

CAS No. 74050-98-9
Storage powder
Synonyms R41468

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02451072 Completed Healthy Psychiatric University Hospital, Zurich March 2015 --
NCT02632877 Completed Diabetic Foot Ulcer University of Guadalajara|Cell Pharma, SA de CV January 2014 Phase 1|Phase 2
NCT01329887 Completed Severe Sepsis|Septic Shock Medical Centre Leeuwarden March 2011 Phase 3
NCT00557219 Terminated Acute Renal Failure Medical University of Gdansk April 2008 Phase 3

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID