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 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 receptor 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 Organization[1] and the National Institute of Health.[2]

Ketanserin 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

  1. ^ ATC/DDD Index
  2. ^ Ketanserin
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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
Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents (including alpha)
Vasodilators
Other antihypertensives
Low ceiling diuretics
High ceiling diuretics
Potassium-sparing diuretics


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  • This page was last modified on 3 July 2008, at 22:53.

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