High affinity and selective 5-HT6 agonist (Ki = 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.
Brouard et al (2015) Pharmacological evidence for 5-HT6 receptor modulation of 5-HT neuron firing in Vivo. ACS Chem.Neurosci. 6 1241 PMID:25837696 |Cole et al (2007) 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. J.Med.Chem. 50 5535 PMID:17948978