| Assay Method Information | |
| | 5-HT2A Receptor Binding Assay |
| Description: | The binding affinities of disclosed compounds at the ketanserin binding site of the 5-HT2A receptor were determined in radioligand binding experiments, with the results summarized in Table 1. Disclosed compounds exhibited substantial binding affinity for the 5-HT2A receptor. The affinity of Compound 1 was much higher than the other pyridine isomer Compound 11 and the pyrazine Compound 12, indicating the preferred positioning of the pyridine nitrogen in the compounds of the invention. Generally, compounds with an ethyl substituent alpha to the basic amine were less potent than compounds bearing a hydrogen or methyl substituent at this position. Longer alkyl or fluoroalkyl substituents at position 5 of the pyridine also tended to increase potency compared to smaller substituents at this position. |
| Affinity data for this assay | |
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