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| Systematic (IUPAC) name | |
|---|---|
| 3-{2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl}quinazoline-2,4(1 H,3H)-dione | |
| Identifiers | |
| CAS number | 74050-98-9 |
| ATC code | C02KD01 QD03 |
| PubChem | 3822 |
| Chemical data | |
| Formula | C 22FN3O3 |
| Mol. mass | 395.43 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. | ? |
| Legal status | |
| Routes | ? |
Ketanserin is drug with affinity for multiple GPCR receptors. Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this not true. Ketanserin only has weak selectivity for 5-HT2A receptors over 5-HT2C receptors (~20-30 fold). Ketanserin also has high affinity for alpha-1 adrenergic receptors, and very high affinity for histamine H1 receptors. Therefore, ketanserin can not be used to reliably discriminate between the effects of 5-HT2A and 5-HT2C receptors when both are present in an experimental system. Furthermore, when alpha-1 and H1 receptors are present, the effects of ketanserin can potentially represent a complex interaction of serotonin, adrenergic, and histamine receptor systems. Complicating the matter further is the fact that ketanserin has moderate affinity for alpha-2 adrenergic (~200 nM) and 5-HT6 (~300 nM) receptors as well as weak affinity for dopamine D1 and D2 receptors (~300 nM and ~500 nM respectively). Ketanserin at levels of 500 nM or greater are thus potentially affecting at least 8 different GPCRs from 4 different families. (All affinity levels taken from the NIMH Psychoactive Drug Screening Program database [1])
Receptors for which ketanserin has high affinity binding:
Ketanserin was discovered at Janssen Pharmaceutica in 1980.
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It is classified as an antihypertensive by the World Health Organization[2] and the National Institute of Health.[3]
It has been used to reverse hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose).[4]
The reduction in hypertension is not associated with reflex tachycardia.[5]
It has been used in cardiac surgery.[6]
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.[7] This radiolabeling enables the study of the serotonin-2A receptor distribution in the human brain.[8]
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).[9] The same research team found no significant correlation with age in their homogenate binding study.
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