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Ketanserin
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| Systematic (IUPAC) name | |
| 3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione | |
| Identifiers | |
| CAS number | |
| ATC code | C02 |
| PubChem | |
| Chemical data | |
| Formula | C22FN3O3 |
| Mol. mass | 395.43 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| 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.
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Uses
Antihypertensive
It is classified as an antihypertensive by the World Health Organization[1] and the National Institute of Health.[2]
It has been used to reverse hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose).[3]
The reduction in hypertension is not associated with reflex tachycardia.[4]
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.[5] This radiolabeling enables the study of the serotonin-2A receptor distribution in the human brain.[6]
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).[7] The same research team found no significant correlation with age in their homogenate binding study.
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References
- ^ 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. 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. PMID 2786422.
- ^ 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:.
- ^ 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:. 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:.
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