AMI-193

AMI-193 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT_2A and the dopamine D₂ receptor.^1,2 It is selective for the 5-HT_2A receptor over 5-HT_2B and 5-HT_1C receptors (K_is = 22.39, 977.24, and 1,548.82 nM, respectively) but does bind to the 5-HT_1A receptor (K_i = 50 nM). It selectively binds to the dopamine D₂ receptor over the dopamine D₁ receptor (K_is = 3 and 2,530 nM, respectively).² AMI-193 (0.05 mg/kg) completely inhibits amphetamine-induced increases in locomotor activity and rearing behavior in rats for at least three hours.³ It also reduces amphetamine-induced increases in locomotor activity and rearing behavior in mice when used at doses of 0.15 and 0.2 mg/kg but the effects only last for 30 minutes.

WARNING This product is not for human or veterinary use.

1. Knight, A.R., Misra, A., Quirk, K., et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT_2A, 5-HT_2B and 5-HT_2C receptors. Naunyn Schmiedebergs Arch. Pharmacol. 370(2), 114-123 (2004).

2. Ismaiel, A.M., De Los Angeles, J., Teitler, M., et al. Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT₂- versus 5-HT_1C-selective antagonist. J. Med. Chem. 36(17), 2519-2525 (1993).

3. Rolinski, Z., and Scheel-Krüger, J. The effect of dopamine and noradrenaline antagonists on amphetamine induced locomotor activity in mice and rats. Acta Pharmacol. Toxicol. (Copenh) 33(5), 385-399 (1973).