Ketanserin

drugbox
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 =
C=22|H22|F=1|N=3|O=3
molecular_weight = 395.43 g/mol
bioavailability =
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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.

Uses

Antihypertensive

It is classified as an antihypertensive by the World Health Organization [ [http://www.whocc.no/atcddd/indexdatabase/index.php?query=C02KD01 ATC/DDD Index ] ] and the National Institute of Health. [ [http://www.nlm.nih.gov/cgi/mesh/2006/MB_cgi?mode=&term=Ketanserin 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=http://bja.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=2786422]

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.

References


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