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 |