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Table 2 Characterization of compounds by heterologous competition binding

From: Dibenzazecine compounds with a novel dopamine/5HT2A receptor profile and 3D-QSAR analysis

Compound

pKi

 

hD1

hD2L

hD3

hD4.4

hD5

h5HT2A

Haloperidol

6.55 ± 0.09

8.56 ± 0.05

8.00 ± 0.05

8.10 ± 0.04

7.50 ± 0.06

6.84 ± 0.12

Clozapine

6.68 ± 0.03

6.60 ± 0.06

6.13 ± 0.05

6.93 ± 0.08

6.50 ± 0.08

8.23 ± 0.07

LE300

7.98 ± 0.06

7.19 ± 0.04

6.48 ± 0.04

6.46 ± 0.08

7.99 ± 0.05

9.65 ± 0.04

LE400

5.58 ± 0.16

5.90 ± 0.05

5.28 ± 0.07

4.79 ± 0.06

5.44 ± 0.07

6.86 ± 0.13

LE401

4.77 ± 0.25

5.06 ± 0.13

4.83 ± 0.16

< 4a)

4.79 ± 0.50

< 4a)

LE403

7.94 ± 0.06

6.43 ± 0.07

6.14 ± 0.10

6.26 ± 0.06

7.84 ± 0.05

8.40 ± 0.08

LE404

8.47 ± 0.10

7.10 ± 0.05

6.73 ± 0.06

7.23 ± 0.03

8.53 ± 0.09

8.79 ± 0.07

LE410

7.76 ± 0.04

7.54 ± 0.06

6.86 ± 0.07

6.32 ± 0.06

7.78 ± 0.10

8.40 ± 0.10

LE420

6.89 ± 0.07

6.64 ± 0.05

6.07 ± 0.06

5.83 ± 0.11

6.92 ± 0.04

7.97 ± 0.05

  1. a) Displacement of radioligand was < 30% at 10 μM
  2. Haloperidol, clozapine, and LE compounds were characterized at dopamine and h5HT2A receptors. [3H]SCH23390 was used for hD1-like and [3H]spiperone for hD2-like and h5HT2A receptors. Displayed are pKi values ± SEM, n ≥ 3.
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BMC Pharmacology

ISSN: 1471-2210