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. 2023 Aug 31;14(9):1216–1223. doi: 10.1021/acsmedchemlett.3c00143

Table 3. Receptor Binding Affinities and Enzyme Inhibition for 9i and 7.

    9i
7
receptor/enzyme ligand IC50 (μM) Ki (μM) nH IC50 (μM) Ki (μM) nH
5-HT1A 1.50 nM [3H] 8-OH-DPAT 0.19 0.11 1.26 0.18 0.10 0.97
5-HT1B 1.0 nM [3H] GR125743 1.99 1.52 0.74 2.42 1.84 0.76
5-HT2A 0.5 nM [3H] ketanserin 0.22 0.06 0.84 0.15 0.04 0.78
5-HT2B 2.0 nM [3H] mesulergine 0.41 0.30 0.98 0.48 0.35 1.08
5-HT2C 1.0 nM [3H] mesulergine 0.39 0.20 0.94 0.53 0.28 1.38
5-HT5A 1.70 nM [3H] lysergic acid diethylamide (LSD) 3.32 1.71 1.01 3.32 1.71 0.91
5-HT6 1.50 nM [3H] lysergic acid diethylamide (LSD) 1.08 0.50 0.77 1.21 0.56 0.84
5-HT7 5.50 nM [3H] lysergic acid diethylamide (LSD) 0.09 0.05 0.67 0.12 0.07 0.91
α1A 0.6 nM [3H] prazosin 0.99 0.48 1.00 0.58 0.28 0.75
α1B 0.2 nM [3H] prazosin 0.93 0.37 0.94 0.67 0.26 0.94
α1D 0.6 nM [3H] prazosin 3.26 1.60 0.73 3.07 1.51 0.85
α2A 1.50 nM [3H] rauwolscine 3.03 1.52 1.00 2.22 1.11 0.76
α2B 2.50 nM [3H] rauwolscine 1.67 0.76 0.97 1.58 0.72 1.09
α2C 0.5 nM [3H] rauwolscine 6.10 2.71 1.03 9.47 4.21 0.56
H1 1.20 nM [3H] pyrilamine 0.34 0.16 0.63 0.52 0.25 1.09
I2, central 2.0 nM [3H] idazoxan 2.60 1.73 0.99 1.93 1.29 0.87
nAChα3β4 0.05 nM [125I] epibatidine 4.40 3.18 0.90 4.20 3.03 0.79
MAO-A   1.50     1.18