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Table 5 Inhibitory potencies of the LE compounds on agonist-induced effects on [cAMP]i, [Ca2+]i, and [35S]-GTPγS binding

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

 

pK i app

Compound

[cAMP]i

[Ca2+]i

[35S]-GTPγ S binding

 

hD1

hD2L

hD1

hD2L

hD1

hD2L

Haloperidol

6.80 ± 0.10

9.88 ± 0.07

6.61 ± 0.09

10.0 ± 0.13

7.10 ± 0.91

9.10 ± 0.07

Clozapine

6.46 ± 0.05

7.30 ± 0.07

6.54 ± 0.15

6.92 ± 0.11

7.47 ± 0.29

7.48 ± 0.08

LE300

7.55 ± 0.13

8.73 ± 0.10

7.22 ± 0.15

7.93 ± 0.12

7.75 ± 0.12

8.14 ± 0.11

LE400

5.35 ± 0.17

6.88 ± 0.09

< 5.00a)

< 5.00a)

6.25 ± 0.13

6.39 ± 0.14

LE401

5.00 ± 0.13

< 5.00a)

< 5.00a)

< 5.00a)

< 5.00a)

< 5.00a)

LE403

7.02 ± 0.09

7.23 ± 0.12

7.57 ± 0.11

7.14 ± 0.08

7.48 ± 0.12

7.20 ± 0.15

LE404

7.95 ± 0.09

8.01 ± 0.08

8.20 ± 0.15

7.71 ± 0.01

8.10 ± 0.13

8.13 ± 0.08

LE410

7.35 ± 0.12

8.63 ± 0.07

7.39 ± 0.07

8.13 ± 0.11

8.02 ± 0.08

8.13 ± 0.09

LE420

6.44 ± 0.21

7.69 ± 0.08

6.73 ± 0.09

7.08 ± 0.12

7.17 ± 0.11

7.51 ± 0.08

  1. a) Inhibitory activity was ≤ 50% at 10 μM.
  2. Concentration-effect curves were obtained with hD1 and hD2L receptors. Data shown are apparent pK i values (pK i app ) ± SEM, n ≥ 3.