WAY-181187

WAY-181187 is an agonist of the serotonin (5-HT) receptor subtype 5-HT₆.^1,2 It increases intracellular cAMP levels in HeLa cells expressing 5-HT₆ (EC₅₀ = 6.5 nM).² WAY-181187 selectively binds to 5-HT₆ over 5-HT_2B, 5-HT_2C, and 5-HT₇ (K_is = 2,458, 124, and 679 nM, respectively). It is also selective for 5-HT₆ over a panel of 31 receptors and ion channels at 100 nM. It increases extracellular GABA levels in the rat frontal cortex when administered at a dose of 10 mg/kg. WAY-181187 (178 mg/kg) reduces schedule-induced polydipsia, an adjunctive model of compulsive disorder, in rats. It also reduces immobility in a modified forced swim test in rats when administered at a dose of 17 mg/kg, indicating antidepressant-like activity, and reduces the duration of defensive burying in rats at 10 and 17 mg/kg, indicating anxiolytic-like activity.³

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1. Schechter, L.E., Lin, Q., Smith, D.L., et al. Neuropharmacological profile of novel and selective 5-HT₆ receptor agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology 33(6), 1323-1335 (2008).

2. Cole, D.C., Stock, J.R., Lennox, W.J., et al. 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(23), 5535-5538 (2007).

3. Carr, G.V., Schechter, L.E., and Lucki, I. Antidepressant and anxiolytic effects of selective 5-HT₆ receptor agonists in rats. Psychopharmacology (Berl) 213(2-3), 499-507 (2011).