Ketanserin

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Ketanserin
Clinical data
ATC code	C02KD01 (WHO) ;
Identifiers
CAS Number	74050-98-9;
PubChem CID	3822;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C22FN3O3
Molar mass	395.43 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Ketanserin (R41468) is a drug with affinity for multiple G protein-coupled receptors (GPCR). It is a highly selective antagonist for serotonin 5-HT_2A receptors, but also has moderate selectivity for 5-HT_2C receptors and for alpha-1 adrenergic receptors, and very high affinity for histamine H1 receptors. Therefore, ketanserin can not be used to reliably discriminate between the effects of 5-HT_2A and 5-HT_2C receptors when both are present in an experimental system. Furthermore, when alpha-1 and H1 receptors are present, the effects of ketanserin can potentially represent a complex interaction of serotonin, adrenergic, and histamine receptor systems. Complicating the matter further is the fact that ketanserin has moderate affinity for delta-1t adrenergic receptor (~200 nM) and 5-HT₆ (~300 nM) receptors as well as weak affinity for dopamine D1 and D2 receptors (~300 nM and ~500 nM respectively). Ketanserin at levels of 500 nM or greater are thus potentially affecting at least 8 different GPCRs from 4 different families. (All affinity levels taken from the NIMH Psychoactive Drug Screening Program database ^[1])

Receptors for which ketanserin has high affinity binding:

5-HT_2A = 2-3 nM (rat and human)
5-HT_2C = 50 nM (rat), 100 nM (human)
alpha-1 adrenergic = ~40 nM
Histamine H1 = 2 nM

Solubility:

6 mg/mL 0.1 M HCl
10 mM H20
3.3 mg/mL ethanol
52 mg/mL DMSO

Ketanserin was discovered at Janssen Pharmaceutica in 1980.

Uses

Antihypertensive

It is classified as an antihypertensive by the World Health Organization^[2] and the National Institute of Health.^[3]

It has been used to reverse hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose).^[4]

The reduction in hypertension is not associated with reflex tachycardia.^[5]

It has been used in cardiac surgery.^[6]

As a Radioligand

With tritium (³H) radioactively labeled ketanserin is used as a radioligand for the serotonin 5-HT_2A receptor, e.g. in receptor binding assays and autoradiography.^[7] This radiolabeling enables the study of the serotonin-2A receptor distribution in the human brain.^[8]

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).^[9] The same research team found no significant correlation with age in their homogenate binding study.

As a Blocker with Another Radioligand

Ketanserin has also been used with carbon (¹¹C) radioactively labeled NNC112 in order to image cortical D₁ receptors without contamination by 5-HT_2A receptors.^[10]

References

↑ NIMH Psychoactive Drug Screening Program
↑ ATC/DDD Index
↑ Ketanserin
↑ van der Starre PJ, Solinas C (1996). "Ketanserin in the treatment of protamine-induced pulmonary hypertension". Texas Heart Institute journal / from the Texas Heart Institute of St. Luke's Episcopal Hospital, Texas Children's Hospital. 23 (4): 301–4. PMC 325377. PMID 8969033.
↑ Hodsman NB, Colvin JR, Kenny GN (May 1989). "Effect of ketanserin on sodium nitroprusside requirements, arterial pressure control and heart rate following coronary artery bypass surgery". British journal of anaesthesia. 62 (5): 527–31. doi:10.1093/bja/62.5.527. PMID 2786422.
↑ Elbers PW, Ozdemir A, van Iterson M, van Dongen EP, Ince C (December 2008). "Microcirculatory Imaging in Cardiac Anesthesia: Ketanserin Reduces Blood Pressure But Not Perfused Capillary Density". J. Cardiothorac. Vasc. Anesth. 23 (1): 95–101. doi:10.1053/j.jvca.2008.09.013. PMID 19058975.
↑ Simon B. Eickhoff, Axel Schleicher, Filip Scheperjans, Nicola Palomero-Gallagher & Karl Zilles (2007). "Analysis of neurotransmitter receptor distribution patterns in the cerebral cortex". NeuroImage. 34 (4): 1317–1330. doi:10.1016/j.neuroimage.2006.11.016. PMID 17182260.
↑ A. Pazos, A. Probst, J. M. Palacios (1987). "Serotonin receptors in the Human Brain—IV. Autoradiographic mapping of serotonin-2 receptors". Neuroscience. 21 (1): 123–139. doi:10.1016/0306-4522(87)90327-7. PMID 3601071.
↑ Sharon L. Eastwood, Philip W. J. Burnet, Rebecca Gittins, Kate Baker, Paul J. Harrison (November 2001). "Expression of serotonin 5-HT_2A receptors in the human cerebellum and alterations in schizophrenia". Synapse. 42 (2): 104–114. doi:10.1002/syn.1106. PMID 11574947.
↑ Catafau AM, Searle GE, Bullich S, Gunn RN, Rabiner EA, Herance R, Radua J, Farre M, Laruelle M. (2010). "Imaging cortical dopamine D1 receptors using 11C NNC112 and ketanserin blockade of the 5-HT 2A receptors". J Cereb Blood Flow Metab. 30: 985–93. doi:10.1038/jcbfm.2009.269.

[1] NIMH Psychoactive Drug Screening Program

[2] ATC/DDD Index

[3] Ketanserin

[pmid8969033-4] van der Starre PJ, Solinas C (1996). "Ketanserin in the treatment of protamine-induced pulmonary hypertension". Texas Heart Institute journal / from the Texas Heart Institute of St. Luke's Episcopal Hospital, Texas Children's Hospital. 23 (4): 301–4. PMC 325377. PMID 8969033.

[pmid2786422-5] Hodsman NB, Colvin JR, Kenny GN (May 1989). "Effect of ketanserin on sodium nitroprusside requirements, arterial pressure control and heart rate following coronary artery bypass surgery". British journal of anaesthesia. 62 (5): 527–31. doi:10.1093/bja/62.5.527. PMID 2786422.

[pmid19058975-6] Elbers PW, Ozdemir A, van Iterson M, van Dongen EP, Ince C (December 2008). "Microcirculatory Imaging in Cardiac Anesthesia: Ketanserin Reduces Blood Pressure But Not Perfused Capillary Density". J. Cardiothorac. Vasc. Anesth. 23 (1): 95–101. doi:10.1053/j.jvca.2008.09.013. PMID 19058975.

[7] Simon B. Eickhoff, Axel Schleicher, Filip Scheperjans, Nicola Palomero-Gallagher & Karl Zilles (2007). "Analysis of neurotransmitter receptor distribution patterns in the cerebral cortex". NeuroImage. 34 (4): 1317–1330. doi:10.1016/j.neuroimage.2006.11.016. PMID 17182260.

[8] A. Pazos, A. Probst, J. M. Palacios (1987). "Serotonin receptors in the Human Brain—IV. Autoradiographic mapping of serotonin-2 receptors". Neuroscience. 21 (1): 123–139. doi:10.1016/0306-4522(87)90327-7. PMID 3601071.

[9] Sharon L. Eastwood, Philip W. J. Burnet, Rebecca Gittins, Kate Baker, Paul J. Harrison (November 2001). "Expression of serotonin 5-HT_2A receptors in the human cerebellum and alterations in schizophrenia". Synapse. 42 (2): 104–114. doi:10.1002/syn.1106. PMID 11574947.

[10] Catafau AM, Searle GE, Bullich S, Gunn RN, Rabiner EA, Herance R, Radua J, Farre M, Laruelle M. (2010). "Imaging cortical dopamine D1 receptors using 11C NNC112 and ketanserin blockade of the 5-HT 2A receptors". J Cereb Blood Flow Metab. 30: 985–93. doi:10.1038/jcbfm.2009.269.

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v t e Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents	Template:Navbox subgroup
Vasodilators	Diazoxide • hydrazinophthalazine (Hydralazine, Dihydralazine, Endralazine, Cadralazine) • Minoxidil • Nitroprusside • Phentolamine
Other antihypertensives	serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan) • MAOI (Pargyline) • THI (Metirosine)
Diuretics	Template:Navbox subgroup