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Table 3 FI, receptor occupancy, plasma exposure in S-D rats administered CE-178253

From: Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) Receptor Antagonist

Dose (mg/kg, p.o.)

Food Intake % decrease (mean ± SEM)

% Receptor Occupancy (mean ± S-D)

Unbound Plasma Concentration (nM ± S-D )

Unbound plasma/rat brain Ki

0.3

6 ± 3

27 ± 12

0.17 ± 0.02

0.4

1

25 ± 11

64 ± 2

1.0 ± 0.3

2.3

3

62 ± 5.2*

78 ± 6

2.7 ± 1.0

6.2

10

75 ± 6.2*

82 ± 2

15.6 ± 1.6

36

  1. *significantly different from veh. p < 0.05
  2. Overnight fasted S-D rats were administered veh. (0.5% MC), or CE-178253-01 p.o. Food was returned 30 min later. Cumulative food consumption was measured 2 hr after the return of food.
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BMC Pharmacology

ISSN: 1471-2210