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. 2009 Jan 12;156(2):338–353. doi: 10.1111/j.1476-5381.2008.00001.x

Table 5.

Efficacy and potency of F15599 and comparators for stimulation of [35S]-GTPγS binding to membranes prepared from various brain regions

Tissue/cell line F15599
F13714
(+)8-OH-DPAT
5-HT
Emax (%) pEC50 Emax (%) pEC50 Emax (%) pEC50 Emax (%) pEC50
Prefrontal cortex 54 ± 3 7.20 ± 0.04 54 ± 6 9.19 ± 0.08 65 ± 2 7.62 ± 0.14 92 ± 5 7.25 ± 0.05
Entorhinal cortex 63 ± 7 7.00 ± 0.14 65 ± 12 9.14 ± 0.01 75 ± 6 7.41 ± 0.05 101 ± 7 7.07 ± 0.08
Hippocampus 78 ± 2 6.85 ± 0.03 77 ± 2 9.02 ± 0.04 77 ± 3 7.59 ± 0.04 101 ± 1 6.99 ± 0.03
Dorsal raphe 68 ± 8 6.42 ± 0.12 64 ± 4 8.73 ± 0.08 n.d. n.d.
Median raphe 57 ± 2 6.62 ± 0.06 57 ± 2 8.82 ± 0.07 n.d. n.d.

Efficacy (Emax) values are expressed as % of the stimulation induced by saturating concentrations (10 µmol·L−1) of 5-HT. Slope values of the [35S]-GTPγS binding isotherms did not significantly differ from unity except in: (i) dorsal raphe F15599 0.62 ± 0.07, F13714 0.76 ± 0.03; (ii) median raphe F13714 0.69 ± 0.03; and (iii) prefrontal cortex (+)8-OH-DPAT 0.59 ± 0.06.

n.d., not determined.