Ketanserin 74050-98-9
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 )
read more [+]| Systematic (IUPAC) name: | 3-2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl}quinazoline-2,4(1H,3H)-dione |
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| Ketanserin CAS number: | 74050-98-9 |
| ATC code: | C02KD01 QD03AX90 |
| PubChem: | 3822 |
| DrugBank: | |
| Formula: | C22FN3O3 |
| Molecular mass: | 395.43 g/mol |
| Ketanserin Assay/Purity: | Typically NLT 98% |
