Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | In stock | $ 30.00 | |
100 mg | In stock | $ 48.00 | |
200 mg | In stock | $ 88.00 | |
500 mg | In stock | $ 143.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 48.00 |
Description | Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation. |
Targets&IC50 | 5-HT2C (rat):50 nM(Ki), 5-HT2A:2.5 nM(Ki), 5-HT2C (human):100 nM(Ki) |
In vitro | In the acetic acid-induced writhing and hot plate tests, ketanserin exhibited dose-dependent analgesic effects in rats, with ED50 values of 0.62 mg/kg and 1.51 mg/kg, respectively; however, it showed no effect on the tail flick test. |
In vivo | Research has demonstrated that Ketanserin reduces both the α1-adrenergic receptor-mediated responses and the excitation caused by norepinephrine in the lateral geniculate nucleus. This effect is indicative of induced inhibition rather than attenuation of 5-HT-mediated responses. In isolated rat tail and carotid arteries, dog basilar, gastric splenic and coronary arteries, as well as canine hidden veins and gastric splenic veins, Ketanserin dose-dependently inhibits the contraction induced by 5-hydroxytryptamine (5-HT). In rat cardiac myocytes, Ketanserin significantly prolongs the action potential duration, with repolarization reaching 218% at 50% and 256% at 90%, without significantly affecting other action potential parameters. Ketanserin inhibits the contraction of canine hidden veins and rat tail arteries induced by the activation of postsynaptic α-adrenergic receptors. In addition, Ketanserin inhibits the contractile response to 5-HT in perfused guinea pig gastric vessels and can reverse the response in some experiments. Ketanserin inhibits the transient outward potassium current (Ito) in a time- and concentration-dependent manner (EC50: 8.3 μM) and also dose-dependently inhibits both Ito and sustained currents (EC50: 11.2 μM), but does not affect L-type calcium currents or inward rectifier potassium currents. |
Cell Research | Ketanserin is dissolved in DMSO to produce a stock solution of 100 mM. Ketanserin stock is diluted in experimental solutions to achieve the final concentrations[1]. The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% foetal bovine serum, 400 μg/mL G418. The HEK 293 cell line stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained in DMEM containing 10% foetal bovine serum and 100 μg/mL hygromycin. Cells used for electrophysiology are seeded on a glass coverslip. The mutant hERG channels are constructed, and are transiently expressed in HEK 293 cells using 10 μL of Lipofectamine 2000 with 4 μg of hERG mutant cDNA in pCDNA3 vector[1]. |
Synonyms | R41468, Ketanserin tartrate, Ketanserinum |
Molecular Weight | 395.43 |
Formula | C22H22FN3O3 |
CAS No. | 74050-98-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9 mg/mL (22.76 mM)
You can also refer to dose conversion for different animals. More
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Ketanserin 74050-98-9 Autophagy GPCR/G Protein Membrane transporter/Ion channel Neuroscience 5-HT Receptor Potassium Channel R 41468 Ketanserin Tartrate KcsA inhibit R41468 R-41468 Ketanserin tartrate Serotonin Receptor Inhibitor 5-hydroxytryptamine Receptor Ketanserinum inhibitor