Ketanserin

Ketanserin

Clinical data
Trade names	Sufrexal
AHFS/Drugs.com	International Drug Names
ATC code	C02KD01 (WHO) QD03AX90 (WHO)
Identifiers
IUPAC name 3-{2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl}quinazoline-2,4(1H,3H)-dione
Synonyms	R41468; R-41468; R-41,468
CAS Number	74050-98-9 Y
PubChem (CID)	3822
IUPHAR/BPS	88
ChemSpider	3690 Y
UNII	97F9DE4CT4 Y
KEGG	D02363 Y
ChEBI	CHEBI:6123 N
ChEMBL	CHEMBL51 Y
ECHA InfoCard	100.070.598
Chemical and physical data
Formula	C22H22FN3O3
Molar mass	395.43 g/mol
3D model (Jmol)	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) Y Key:FPCCSQOGAWCVBH-UHFFFAOYSA-N Y
NY (what is this?)

Ketanserin (INN, USAN, BAN) (brand name Sufrexal; former developmental code name R41468) is a drug used clinically as an antihypertensive agent and in scientific research to study the serotonin system; specifically, the 5-HT₂ receptor family. It was discovered at Janssen Pharmaceutica in 1980.

Ketanserin is classified as an antihypertensive by the World Health Organization and the National Institute of Health.

It has been used to reverse pulmonary hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose).

The reduction in hypertension is not associated with reflex tachycardia.

It has been used in cardiac surgery.

With tritium (³H) radioactively labeled ketanserin is used as a radioligand for serotonin 5-HT₂ receptors, e.g. in receptor binding assays and autoradiography. This radio-labeling has enabled the study of serotonin 5-HT_2A receptor distribution in the human brain.

An autoradiography study of the human cerebellum has found an increasing binding of ³H-ketanserin with age (from below 50 femtomol per milligram tissue at around 30 years og age to over 100 above 75 years). The same research team found no significant correlation with age in their homogenate binding study.