Ketanserin

Ketanserin
Clinical data
Trade names	Sufrexal, Serefrex
Other names	R-41468; R41468; R-41,468; KJK-945; R-49945; R49945
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
Drug class	Serotonin 5-HT2A receptor antagonist
ATC code	C02KD01 (WHO) QD03AX90 (WHO);
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	50%
Protein binding	95% (mainly albumin)
Metabolism	Extensive
Metabolites	• Ketanserin-ol
Onset of action	TmaxTooltip Time to peak levels: 0.53–2.3 hours (range 0.25–5.0 hours)
Elimination half-life	3.5–29 hours
Excretion	Urine; 2% unchanged
Identifiers
	IUPAC name 3-{2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl}quinazoline-2,4(1H,3H)-dione;
CAS Number	74050-98-9 ;
PubChem CID	3822;
IUPHAR/BPS	88;
DrugBank	DB12465 ;
ChemSpider	3690 ;
UNII	97F9DE4CT4;
KEGG	D02363 ;
ChEBI	CHEBI:6123 ;
ChEMBL	ChEMBL51 ;
CompTox Dashboard (EPA)	DTXSID3023188 ;
ECHA InfoCard	100.070.598
Chemical and physical data
Formula	C22H22FN3O3
Molar mass	395.434 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c1ccc2c(c1)c(=O)n(c(=O)[nH]2)CCN3CCC(CC3)C(=O)c4ccc(cc4)F;
	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) ; Key:FPCCSQOGAWCVBH-UHFFFAOYSA-N ;
	(verify)

Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospastic disorders. It is also used in scientific research as an antiserotonergic agent in the study of the serotonin system; specifically, the 5-HT₂ receptor family. The drug is taken orally.

Side effects of ketanserin include dizziness, tiredness, edema, dry mouth, weight gain, and QT interval prolongation. Ketanserin acts as a selective antagonist of the serotonin 5-HT_2A, α₁-adrenergic, and histamine H₁ receptors. It also shows lower affinity for various other targets.

Ketanserin was discovered at Janssen Pharmaceutica in 1980. It was the first serotonin 5-HT_2A receptor antagonist to be discovered that showed selectivity over other serotonin receptors. The drug is not available in the United States and is mostly no longer marketed throughout the rest of the world.