AS-19

AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT₇ (K_i = 0.6 nM).¹ It is selective for 5-HT₇ over 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_5A receptors (K_is = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I₂ receptors (K_is = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.² It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT₇ receptor antagonist SB-269970 (Item No. 17081).³

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1. Brenchat, A., Romero, L., García, M., et al. 5-HT₇ receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain 141(3), 239-247 (2009).

2. Perez-García, G.S., and Meneses, A. Effects of the potential 5-HT₇ receptor agonist AS 19 in an autoshaping learning task. Behav. Brain Res. 163(1), 136-140 (2005).

3. Li, S.-F., Zhang, Y.-Y., Li, Y.-Y., et al. Antihyperalgesic effect of 5-HT₇ receptor activation on the midbrain periaqueductal gray in a rat model of neuropathic pain. Pharmacol. Biochem. Behav. 127, 49-55 (2014).