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20-September-2008 09:55:49 - Ketanserin Ketanserin Systematic IUPAC name 3-2-4-4-fluorobenzoylpiperidin-1-ylethyl-1H-quinazoline-2,4-dione Identifiers CAS number 74050-98-9 ATC code C02KD01 PubChem 3822 Chemical data Formula C22FN3O3 Mol. mass 395.43 g/mol Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? 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 Organization1 and the National Institute of Health.2 Use 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.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. 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. doi:10.1016/j.neuroimage.2006.11.016. ^ 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:10.1016/0306-45228790327-7. PMID 3601071. ^ Sharon L. Eastwood, Philip W. J. Burnet, Rebecca Gittins, Kate Baker, Paul J. Harrison November 2001. Expression of serotonin 5-HT2A receptors in the human cerebellum and alterations in schizophrenia. Synapse 42 2: 104-114. doi:10.1002/syn.1106. v d e Serotonin antagonists 5-HT2 Melperone - Paliperidone - Risperidone - Sertindole - Ziprasidone 5-HT3 Alosetron - Azasetron - Bemesetron - Cilansetron - Dolasetron - Granisetron - Lerisetron - Ondansetron - Palonosetron - Ramosetron - Tropisetron - Zacopride - Zatosetron Other/ungrouped Amperozide - Blonanserin - Bufotenin - Cianopramine - Cinanserin - Clozapine - Cyanopindolol - Cyproheptadine - Deramciclane - Dotarizine - Fananserin - Fenclonine - Ketanserin - Lysergic acid diethylamide - Metergoline - Methiothepin - Methysergide - Mianserin - N,N-Dimethyltryptamine - Nafronyl - Olanzapine - Pindolol - Pipamperone - Pizotyline - Quetiapine - Renzapride - Ritanserin - Sarpogrelate - Setoperone - Tolfenamic acid - Wortmannin - Xylamidine v d e Antihypertensives C02 and diuretics C03 Sympatholytic agents Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz 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 Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone This medical treatment article is a stub. Tablets This pharmacology-related article is a stub. Retrieved from http://en..org/wiki/Ketanserin Categories: Medical treatment stubs | Pharmacology stubs | Drugs Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages 日本語 This page was last modified on 24 July 2008, at 12:4
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