GR46611

GR46611 is an agonist of the serotonin (5-HT) receptor subtype 5-HT_1D.¹ It induces cAMP accumulation in CHO cells expressing the human receptor when used at a concentration of 10 µM. It also binds to 5-HT_1A and 5-HT_1B receptors (K_is = 1.3 and 0.2 nM, respectively). GR46611 (50 µmol/kg) induces hypothermia and decreases hypothalamus and prefrontal cortex levels of 5-hydroxyindoleacetic acid (5-HIAA) in guinea pigs. It potentiates increases in locomotor activity induced by buspirone or 8-hydroxy DPAT (Item No. 22608) in guinea pigs when administered at a dose of 2.5 mg/kg.² GR46611 decreases the number of conditioned responses in an autoshaping learning task in mice when administered after training at a dose of 10 mg/kg, indicating impaired memory consolidation.³

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1. Barf, T.A., de Boer, P., Wikström, H., et al. 5-HT_1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. J. Med. Chem. 39(24), 4717-4726 (1996).

2. O'Neill, M.F., and Sanger, G.J. GR46611 potentiates 5-HT_1A receptor-mediated locomotor activity in the guinea pig. Eur. J. Pharmacol. 370(2), 85-92 (1999).

3. Meneses, A., Terrón, J.A., and Hong, E. Effects of the 5-HT receptor antagonists GR127935 (5-HT_1B/1D) and MDL100907 (5-HT_2A) in the consolidation of learning. Behav. Brain Res. 89(1-2), 217-223 (1997).