This is the first study to demonstrate that E-6801, a potent 5-HT(6) receptor agonist, improves recognition memory by combined modulation of cholinergic and glutamatergic neurotransmission.
3 From electrophysiological studies in rat raphe slices in vitro, SB-272183 did not e ect cell ®ring rate up to 1 mM but was able to attenuate (+)8-OH-DPAT-induced inhibition of cell ®ring to give an apparent pK b of 7.1. 4 SB-272183 potentiated electrically-stimulated [ 3 H]-5-HT release from rat and guinea-pig cortical slices at 100 and 1000 nM, similar to results previously obtained with the 5-HT 1B and 5-HT 1D receptor antagonist, GR127935. 5 Fast cyclic voltammetry studies in rat dorsal raphe nucleus showed that SB-272183 could block sumatriptan-induced inhibition of 5-HT e ux, with an apparent pK b of 7.2, but did not e ect basal e ux up to 1 mM. 6 These studies show that, in vitro, SB-272183 acts as an antagonist at native tissue 5-HT 1A , 5-HT 1B and 5-HT 1D receptors.
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