Ketanserin (tartrate)

Ketanserin is a potent antagonist of the serotonin (5-HT) receptor that is selective for 5-HT2 (IC50 = 6.3 nM, Ki = 2.1 nM). It has no activity at 5-HT1 receptors but does have activity at histamine type 1, alpha1-adrenergic, and dopamine receptors with Ki values of 10, 10, and 220 nM, respectively. Ketanserin induces dose-dependent inhibition of contractile responses to 5-HT in isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, and canine gastrosplenic and saphenous veins. Ketanserin (10 mg/kg/day) significantly decreases blood pressure (BP), blood pressure variability (BPV), and hypertensive organ damage in spontaneously hypertensive rats. Formulations containing ketanserin have been used to treat hypertension in early-onset preeclampsia.Formal Name: 3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,4(1H,3H)-quinazolinedione (2R,3R)-2,3-dihydroxybutanedioate. CAS Number: 83846-83-7. Molecular Formula: C22H22FN3O3 . C4H6O6. Formula Weight: 545.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml. lambdamax: 219, 244 nm. SMILES: O=C1N(CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)C(C4=CC=CC=C4N1)=O.OC([C@H](O)[C@@H](O)C(O)=O)=O. InChi Code: InChI=1S/C22H22FN3O3.C4H6O6/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)29,5-1(3(7)8)2(6)4(9)10/h1-8,16H,9-14H2,(H,24,29),1-2,5-6H,(H,7,8)(H,9,10)/t,1-,2-/m.1/s1. InChi Key: KMTLTEVOQLMYRS-LREBCSMRSA-N.