IUPAC_name = 3- [2- [4-(4-fluorobenzoyl)piperidin-1-yl] ethyl] -1"H"-quinazoline-2,4-dione

CAS_number = 74050-98-9
ATC_prefix = C02
ATC_suffix = KD01
PubChem = 3822
DrugBank =
chemical_formula =
molecular_weight = 395.43 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
excretion =
pregnancy_AU =
pregnancy_US =
legal_AU =
legal_CA =
legal_UK =
legal_US =
legal_status =
routes_of_administration =

Ketanserin is a serotonin antagonist.It has the highest affinity for the serotonin 5-HT2A receptor, but also binds less potently to the 5-HT2C, 5-HT2B, 5-HT1D, alpha-adrenergic, and dopamine receptors.

Ketanserin was discovered at Janssen Pharmaceutica in 1980.



It is classified as an antihypertensive by the World Health Organization [ [ ATC/DDD Index ] ] and the National Institute of Health. [ [ Ketanserin ] ]

It has been used to reverse hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose).cite journal |author=van der Starre PJ, Solinas C |title=Ketanserin in the treatment of protamine-induced pulmonary hypertension |journal=Texas Heart Institute journal / from the Texas Heart Institute of St. Luke's Episcopal Hospital, Texas Children's Hospital |volume=23 |issue=4 |pages=301–4 |year=1996 |pmid=8969033 |pmc=325377 |doi= |url=]

The reduction in hypertension is not associated with reflex tachycardia.cite journal |author=Hodsman NB, Colvin JR, Kenny GN |title=Effect of ketanserin on sodium nitroprusside requirements, arterial pressure control and heart rate following coronary artery bypass surgery |journal=British journal of anaesthesia |volume=62 |issue=5 |pages=527–31 |year=1989 |month=May |pmid=2786422 |doi= |url=]

As a radioligand

With tritium (3H) radioactively labeled ketanserin is used as a radioligand for the serotonin 5-HT2A receptor, e.g. in receptor binding assays and autoradiography. [Cite journal
author = Simon B. Eickhoff, Axel Schleicher, Filip Scheperjans, Nicola Palomero-Gallagher & Karl Zilles
title = Analysis of neurotransmitter receptor distribution patterns in the cerebral cortex
journal = NeuroImage
year = 2007
volume = 34
pages = 1317–1330
doi = 10.1016/j.neuroimage.2006.11.016
] This radiolabeling enables the study of the serotonin-2A receptor distribution in the human brain. [Cite journal
author = A. Pazos, A. Probst, J. M. Palacios
title = Serotonin receptors in the Human Brain—IV. Autoradiographic mapping of serotonin-2 receptors
journal = Neuroscience
volume = 21
issue = 1
pages = 123–139
pmid = 3601071
doi = 10.1016/0306-4522(87)90327-7
year = 1987

An autoradiography study of the human cerebellum has found an increasing binding of H-3-ketanserin with age (from below 50 femtomol per milligram tissue at around 30 years og age to over 100 above 75 years). [Cite journal
author = Sharon L. Eastwood, Philip W. J. Burnet, Rebecca Gittins, Kate Baker, Paul J. Harrison
title = Expression of serotonin 5-HT2A receptors in the human cerebellum and alterations in schizophrenia
journal = Synapse
volume = 42
issue = 2
pages = 104–114
month = November
year = 2001
doi = 10.1002/syn.1106
] The same research team found no significant correlation with age in their homogenate binding study.


Wikimedia Foundation. 2010.

Look at other dictionaries:

  • Ketanserin — Strukturformel Allgemeines Freiname Ketanserin Andere Namen …   Deutsch Wikipedia

  • ketanserin — noun A serotonin antagonist …   Wiktionary

  • ketanserin — Specific serotonin 5HT2 receptor antagonist with antihypertensive properties; the drug also reduces platelet aggregation produced by serotonin …   Medical dictionary

  • KFC — Ketanserin for Carcinoid [trial]; Ketanserin on Fibroblast Culture [study] …   Medical dictionary

  • KFC — • Ketanserin for Carcinoid [trial]; • Ketanserin on Fibroblast Culture [study] …   Dictionary of medical acronyms & abbreviations

  • Monoamine oxidase inhibitor — MAOI redirects here. For the Easter Island statues, see Moai. Monoamine oxidase Monoamine oxidase inhibitors (MAOIs) are a class of antidepressant drugs prescribed for the treatment of depression. They are particularly effective in treating… …   Wikipedia

  • Propranolol — Systematic (IUPAC) name …   Wikipedia

  • Oxprenolol — Systematic (IUPAC) name (RS) 1 [2 (allyloxy)phenoxy] 3 (isopropylamino)propan 2 ol Clinical data AHFS/ …   Wikipedia

  • Methyldopa — Systematic (IUPAC) name (S) 2 amino 3 (3,4 dihydroxyphenyl) 2 methyl propanoic acid Clinical data …   Wikipedia

  • Reserpine — Systematic (IUPAC) name methyl 11,17α dimethoxy 18β [(3,4,5 trimethoxybenzoyl) Clinical data AHFS/ …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”

We are using cookies for the best presentation of our site. Continuing to use this site, you agree with this.