High affinity and selective 5-HT6
= 2.2 nM). Displays 60-fold selectivity over other 5-HT and monoamine receptors. Increases firing rate of 5-HT neurons. Modifies sleep and wakefulness profiles following direct injections into the dorsal raphe nucleus, in vivo
. Orally bioavailable.
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Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT6 receptor agonist.
Cole et al.
Pharmacological evidence for 5-HT6 receptor modulation of 5-HT neuron firing in Vivo.
Brouard et al.
ACS Chem.Neurosci., 2015;6:1241