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Ketanserin


Ketanserin
Systematic (IUPAC) name
?
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. With tritium radioactively labeled ketanserin is used as a radioligand for the serotonin 5-HT_2A receptor, e.g. in receptor binding assays.

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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]

References

^ http://www.whocc.no/atcddd/indexdatabase/index.php?query=C02KD01
^ http://www.nlm.nih.gov/cgi/mesh/2006/MB_cgi?mode=&term=Ketanserin

v • d • e Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents (including alpha)	centrally acting/antiadrenergics (Clonidine, Guanfacine, Methyldopa, Moxonidine, Rescinnamine, Reserpine, Rilmenidine) • 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)