Ketanserin

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Ketanserin
Systematic (IUPAC) name
3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione
Identifiers
CAS number	74050-98-9
ATC code	C02KD01
PubChem	3822
Chemical data
Formula	C₂₂F N₃O₃
Mol. mass	395.43 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Ketanserin is a serotonin receptor antagonist. It has the highest affinity for the serotonin 5-HT_2A receptor, but also binds less potently to the 5-HT_2C, 5-HT_2B, 5-HT_1D, alpha-adrenergic, and dopamine receptors.

Ketanserin was discovered at Janssen Pharmaceutica in 1980.

It is classified as an antihypertensive by the World Health Organization^[1] and the National Institute of Health.^[2]

[edit] Ketanserin 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.^[3] This radiolabeling enables the study of the serotonin-2A receptor distribution in the human brain.^[4]

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).^[5] The same research team found no significant correlation with age in their homogenate binding study.

[edit] References

^ ATC/DDD Index
^ Ketanserin
^ 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: 1317–1330.
^ 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.

v • d • e Antihypertensives (C02) and diuretics (C03)

Sympatholytic agents (including alpha)	centrally acting/antiadrenergics: Clonidine • Guanfacine • Methyldopa • Moxonidine • Rilmenidine • adrenergic uptake inhibitor (Rescinnamine, Reserpine) ganglion-blocking/nicotinic antagonist (Mecamylamine, Trimethaphan) peripherally acting/antiadrenergics (Prazosin, Guanethidine, Indoramin, Doxazosin)

Vasodilators	Diazoxide • Hydralazine • Minoxidil • Nitroprusside • Phentolamine

Other antihypertensives	serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan)

Low ceiling diuretics	Thiazide (Bendroflumethiazide, Chlorothiazide, Hydrochlorothiazide) • Chlortalidone • Indapamide • Quinethazone • Mersalyl • Metolazone • Theobromine • Cicletanine

High ceiling diuretics	Loop diuretic (Bumetanide, Furosemide, Torasemide)

Potassium-sparing diuretics	ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)