Ketanserin

SKU: orb1309882

Description

Ketanserin is a selective 5-HT2A receptor antagonist of the quinazoline class. It is widely used in cardiovascular research to study serotonin-mediated vasoconstriction and platelet aggregation in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 74050-98-9
• MW: 395.43
• Purity: 99.73% (May vary between batches)
• Formula: C₂₂H₂₂FN₃O₃
• SMILES: FC1=CC=C(C=C1)C(=O)C1CCN(CCN2C(=O)NC3=CC=CC=C3C2=O)CC1
• Target: Autophagy,5-HT Receptor,Potassium Channel
• Solubility: DMSO:18.52 mg/mL (46.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.53 mM)

Bioactivity

• Target IC50:
  5-HT2C (rat):50 nM(Ki)|ERG current (human):0.11 μM|5-HT2A:2.5 nM(Ki)|5-HT2C (human):100 nM(Ki)
• 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.
• 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.
• 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PotassiumChannel, R41468, R-41468, R 41468, Potassium Channel, Ketanserinum, Ketanserin, 5HT Receptor, 5HTReceptor, 5-HT Receptor, 5-HT2A, 5-HT2C (Human), 5-HT2C (Rat), Autophagy

Compound Identifiers

PubChem CID

3822