Ketanserin

• CAT Number: A000830
• CAS Number: 74050-98-9
• Molecular Formula: C22H22FN3O3
• Molecular Weight: 395.434
• Purity: ≥95%
• Target: 5-HT Receptor
• Solubility: Limited solubility
• Storage: 3 years -20C powder
• IUPAC Name: 3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione
• InChI: InChI=1S/C22H22FN3O3/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)
• InChIKey: FPCCSQOGAWCVBH-UHFFFAOYSA-N
• SMILES: C1CN(CCC1C(=O)C2=CC=C(C=C2)F)CCN3C(=O)C4=CC=CC=C4NC3=O

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.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.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.