. 2023 Apr 4;14(8):1474–1489. doi: 10.1021/acschemneuro.3c00033

Table 1. Radioligand Binding Affinity of 1–5, 6–10, and 16–20 for 5-HT₆ Receptor and the Muscimol Site of the GABA-A Receptor: Antagonistic Activity at 5-HT₆R (K_B) and Electrophysiological Studies of the Selected Compounds.

The values of affinity are expressed as K_i and ± SEM and were determined from minimum three experiments conducted in duplicate. Competitive replacement of [³H]-LSD was used to measure the affinities for the 5-HT₆ receptor.

The outcomes were standardized as a percentage of the maximum reaction observed in the absence of the antagonist.

Competitive replacement of [³H]muscimol was used to establish the affinities for the GABA-A receptor.

The electrophysiological studies examined the agonist mode of tested compounds at a concentration of 10 μM. Results are represented by the GABA current amplitude normalized to 10 μM GABA-induced response (10 μM). n.a.: “not active”. Blank spaces: not tested.

Table 1. Radioligand Binding Affinity of 1–5, 6–10, and 16–20 for 5-HT6 Receptor and the Muscimol Site of the GABA-A Receptor: Antagonistic Activity at 5-HT6R (KB) and Electrophysiological Studies of the Selected Compounds.

Table 1. Radioligand Binding Affinity of 1–5, 6–10, and 16–20 for 5-HT₆ Receptor and the Muscimol Site of the GABA-A Receptor: Antagonistic Activity at 5-HT₆R (K_B) and Electrophysiological Studies of the Selected Compounds.