Inhibition of brain FAAH activity by analogues of 3 bearing
different substituents on the meta- position of the distal
phenyl ring; a) Dose-dependent effects of secondary (7c), tertiary
(7d) or reverse (7e) amide derivatives of compound
3 in Swiss Webster mice; doses were 0.3–40 mg/kg
(subcutaneous); FAAH activity was measured ex vivo 1 h after
injection; b) Dose-dependent effects of sulfonamide (7f) and
methylsulfone (7g) derivatives of compound 3 in Swiss
Webster mice; doses were 0.3–75 mg/kg (s.c.); c) Effects of
pharmacological blockade of the Abcg2 transporter (Ko-143, 15 mg/kg, i.p.,
closed bars) on brain inhibition of FAAH activity by a sub-effective dose
(selected from the dose-response study: 3 (25); 7d
(10); 7e (1); 7f (40); 7g (1) in mg/kg,
s.c., open bars) of analogues of compound 3 bearing different
functionalities on the meta- position of the distal phenyl
ring. Results are expressed as mean ± s.e.m. (n = 3-4). ***
P< 0.001 vs non-Ko-143 treated
group.